5 résultat(s) recherche sur le tag 'biological activity'    

Comportements biologique, physiologique, biochimique et l’activité biologique de quatre variétés d’olivier (Olea europeae L.) dans l’Est Algérien. / Sara Himour ép Cherrier  

Public ISBD Titre : Comportements biologique, physiologique, biochimique et l’activité biologique de quatre variétés d’olivier (Olea europeae L.) dans l’Est Algérien. Type de document : texte imprimé Auteurs : Sara Himour ép Cherrier, Auteur ; Abdelouahab Yahia, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2018 Importance : 209 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Biologie Tags : Olea europaea L.  morphologie  physiologie  HPLC  Oleuropéine  activité biologique  antioxydante  anticoagulante  antibactérienne  morphology  physiology  Oleuropein  biological activity  antioxidant  anticoagulant  antibacterial  ????????????  L??????????? ??????????  HPLC??????????  ?????? ?????????  ?????? ???????  ???? ??????  ???? ????????? Index. décimale : 570 Sciences de la vie. Biologie Résumé : The present study focuses on the biological, physiological and biochemical behavior of the cultivated olive tree, Olea europaea L., represented by four varieties sampled at the Maazouzi Lakhdar station, Mila: Sigoise, Rougette, Chemlel and Dathier. The morphological characterizations (quantitative and qualitative), relating to the leaves, fruits and cores, described in the descriptors of the International Olive Council (IOC, 2003), revealed differences between the varieties. The set of morphological traits assessed during the three years of study (2013-2014- 2015) revealed a significant difference between the varieties studied confirmed by coefficients of variation ranging from 2.81% to 39.14%. Positive correlations between mean precipitation, duration of insolations and morphological characters ranged from r = 0.839 to 0.946, and negative for fruit width and nuclei with temperature. The results of the analysis of the biochemical characterization data revealed a great difference between the varieties. The most important lipid content was recorded in Sigoise leaf and fruit, Rougette gave the best sugar content in the leaves, as well as in Chemlel fruits. The qualitative analysis performed by phytochemical screening revealed the presence of several families of natural compounds in both organs. Rougette has been the dominant variety for total leaf and fruit phenol and flavonoid content, and Dathier for tannins. Quantitative analyzes of the phenolic compounds identified in the hydromethanol extracts by HPLC identified four compounds: fumaric acid, gallic acid, oleuropein and caffeic acid, seven compounds in the leaves: fumaric acid, gallic acid, oleuropein, 4-hydroxybenzoic acid acid, caffeic acid, ellagic acid and t-3 hydroxyroamic acid, with a significant dominance of Oleuropein. The evaluation of the biological potential of leaf and fruit extracts, revealed a significant anticoagulant activity in Chemlel for both organs and an antioxidant power of interest in Rougette leaves and Sigois fruits. All extracts have an important antibacterial power, extracts of leaf at Rougette gave a better zone of inhibition against S. aureus. Diplôme : Doctorat en sciences En ligne : ../theses/biologie/HIM7315.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10931 Comportements biologique, physiologique, biochimique et l’activité biologique de quatre variétés d’olivier (Olea europeae L.) dans l’Est Algérien. [texte imprimé] / Sara Himour ép Cherrier, Auteur ; Abdelouahab Yahia, Directeur de thèse . - [S.l.] : جامعة الإخوة منتوري قسنطينة, 2018 . - 209 f. ; 30 cm. 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Biologie Tags : Olea europaea L.  morphologie  physiologie  HPLC  Oleuropéine  activité biologique  antioxydante  anticoagulante  antibactérienne  morphology  physiology  Oleuropein  biological activity  antioxidant  anticoagulant  antibacterial  ????????????  L??????????? ??????????  HPLC??????????  ?????? ?????????  ?????? ???????  ???? ??????  ???? ????????? Index. décimale : 570 Sciences de la vie. Biologie Résumé : The present study focuses on the biological, physiological and biochemical behavior of the cultivated olive tree, Olea europaea L., represented by four varieties sampled at the Maazouzi Lakhdar station, Mila: Sigoise, Rougette, Chemlel and Dathier. The morphological characterizations (quantitative and qualitative), relating to the leaves, fruits and cores, described in the descriptors of the International Olive Council (IOC, 2003), revealed differences between the varieties. The set of morphological traits assessed during the three years of study (2013-2014- 2015) revealed a significant difference between the varieties studied confirmed by coefficients of variation ranging from 2.81% to 39.14%. Positive correlations between mean precipitation, duration of insolations and morphological characters ranged from r = 0.839 to 0.946, and negative for fruit width and nuclei with temperature. The results of the analysis of the biochemical characterization data revealed a great difference between the varieties. The most important lipid content was recorded in Sigoise leaf and fruit, Rougette gave the best sugar content in the leaves, as well as in Chemlel fruits. The qualitative analysis performed by phytochemical screening revealed the presence of several families of natural compounds in both organs. Rougette has been the dominant variety for total leaf and fruit phenol and flavonoid content, and Dathier for tannins. Quantitative analyzes of the phenolic compounds identified in the hydromethanol extracts by HPLC identified four compounds: fumaric acid, gallic acid, oleuropein and caffeic acid, seven compounds in the leaves: fumaric acid, gallic acid, oleuropein, 4-hydroxybenzoic acid acid, caffeic acid, ellagic acid and t-3 hydroxyroamic acid, with a significant dominance of Oleuropein. The evaluation of the biological potential of leaf and fruit extracts, revealed a significant anticoagulant activity in Chemlel for both organs and an antioxidant power of interest in Rougette leaves and Sigois fruits. All extracts have an important antibacterial power, extracts of leaf at Rougette gave a better zone of inhibition against S. aureus. Diplôme : Doctorat en sciences En ligne : ../theses/biologie/HIM7315.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10931

Exemplaires (1)

Code-barres	Cote	Support	Localisation	Section	Disponibilité
HIM/7315	HIM/7315	Thèse	Bibliothèque principale	Thèses	Disponible

Etudes phytochimique et pharmacologique d’une plante saharienne et d’espèces de la région des Aurès. / Hamza Fadel  

Public ISBD Titre : Etudes phytochimique et pharmacologique d’une plante saharienne et d’espèces de la région des Aurès. Type de document : texte imprimé Auteurs : Hamza Fadel, Auteur ; Samir Benayache, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2018 Importance : 255 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : Pulicaria inuloides  Cistus albidus  les Aurès  fractionnement bioguidé  activité biologique  flavonoïdes  huiles essentielles  ICP-AES et ICP-MS  Aures  bioguided fractionation  biological activity  flavonoids  essential oils  Pulicaria inuloides???????  ???????? ??????????  ????? ?????? ????????  ?????? ???????  ??????? ?????? ???????? ????? )  (ICP-AES??????? ?????? ?????? )(. ICP-M" Index. décimale : 540 Chimie et sciences connexes Résumé : Our goal in this work was to search the secondary metabolites of flavonoids type from two species from Asteraceae and Cistaceae families in order to search new natural compounds of biological interest. Thirteen (13) extracts from different species including twelve (12) from the Aures regions were subjected to a phytochemical screening. On the basis of these preliminary results, the phytochemical investigation of the aerial parts two species, Pulicaria inuloides and Cistus albidus from the Bechar and the Aures regions respectively was carried out. This approach allowed the isolation of twelve natural compounds, among which eleven flavonoids, one phenolic compound as well as two acetyl derivatives of one of the isolated compounds were characterized using spectroscopic methods such as UV-Visible, IR and NMR. The biological activities in vitro (antioxidant and antibacterial activity) as well as the total phenolic and flavonoids compounds of the various extracts were discussed. We also reported the evaluation of the in vitro antiprotozoal activity of the two species Pulicaria inuloides and Cistus albidus against Leishmania amazonensis, Trypanosoma cruzi and Acanthamoeba castellanii str. Neff. The bioguided fractionation of the CHCl3 extract from the aerial part of P. inuloides leads to the isolation and characterization of quercetagetin-3,5,7,3'-tetramethylether as the active ingredient. Two acetylated derivatives were prepared from this natural compound and these three compounds were evaluated for their activities against the promastigote form of L. amazonensis. All these compounds exhibited moderate leishmanicidal activity with IC50 values ranging from 0.234 to 0.484 mM and low toxicity to macrophage cells (CC50 ranging from 0.365 to 0.664 mM). This study reported the antiprotozoal evaluation of Pulicaria inuloides for the first time and the results show that this species can be considered as a source of anti-leishmanicidal agents. The bioguided fractionation of the active extract of CHCl3 from C. albidus against T. cruzi led to the isolation of two fractions F6,4 and F6,5 which showed also a potent activity up to 100 μg/ml. The bioguided fractionation of the active extract of AcOEt from the aerial part of C. albidus against A. castellanii led to the isolation of a fraction F14A which showed a significant activity up to 100 μg / ml. Fractions F6,4 ; F6,5 and F14A consists of product mixtures, which have not been separated. We have also described the chemical compositions of the essential oils of Pulicaria inuloides and Cistus albidus. The major compounds of the species C. albidus are manool and 15,16-dinorlabd-8(20)- en-13-one whose skeleton of type labdane is a specific marker in this genus, these compounds are not described in samples from other regions and in particular in the Mediterranean regions (Spain and France) that appeared in the literature. The major compounds of the species Pulicaria inuloides are: δ- cadinene, α-muurolene, γ-cadinene, α-epi-cadinol and α-cadinol are not present in the other samples of Pulicaria inuloides from other areas published in the literature. In this study, the mineral content (inorganic elements) of 21 isolated extracts of various aromatic species of the Sahara (P. inuloides) and the Aures region (Euphorbia helioscopia L., Peganum harmala L., Daphne gnidium L., Calendula algeriensis L., Bunium incrassatum L., Echinops ritro L. Marrubium deserti de Noè., Juniperus oxycedrus L., Juniperus phoenicea L., Marrubium vulgare L., Cedrus atlantica (Endl.) Manetti and Thymus algeriensis L.) were also determined by inductively coupled plasma atomic emission spectroscopy (ICP-AES) and inductively coupled plasma mass spectroscopy (ICP-MS) . The results obtained showed higher concentrations of Ca, K, Mg, Na and S (mg/kg) in the different plant extracts. Diplôme : Doctorat En ligne : ../theses/chimie/FAD7287.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10902 Etudes phytochimique et pharmacologique d’une plante saharienne et d’espèces de la région des Aurès. [texte imprimé] / Hamza Fadel, Auteur ; Samir Benayache, Directeur de thèse . - [S.l.] : جامعة الإخوة منتوري قسنطينة, 2018 . - 255 f. ; 30 cm. 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : Pulicaria inuloides  Cistus albidus  les Aurès  fractionnement bioguidé  activité biologique  flavonoïdes  huiles essentielles  ICP-AES et ICP-MS  Aures  bioguided fractionation  biological activity  flavonoids  essential oils  Pulicaria inuloides???????  ???????? ??????????  ????? ?????? ????????  ?????? ???????  ??????? ?????? ???????? ????? )  (ICP-AES??????? ?????? ?????? )(. ICP-M" Index. décimale : 540 Chimie et sciences connexes Résumé : Our goal in this work was to search the secondary metabolites of flavonoids type from two species from Asteraceae and Cistaceae families in order to search new natural compounds of biological interest. Thirteen (13) extracts from different species including twelve (12) from the Aures regions were subjected to a phytochemical screening. On the basis of these preliminary results, the phytochemical investigation of the aerial parts two species, Pulicaria inuloides and Cistus albidus from the Bechar and the Aures regions respectively was carried out. This approach allowed the isolation of twelve natural compounds, among which eleven flavonoids, one phenolic compound as well as two acetyl derivatives of one of the isolated compounds were characterized using spectroscopic methods such as UV-Visible, IR and NMR. The biological activities in vitro (antioxidant and antibacterial activity) as well as the total phenolic and flavonoids compounds of the various extracts were discussed. We also reported the evaluation of the in vitro antiprotozoal activity of the two species Pulicaria inuloides and Cistus albidus against Leishmania amazonensis, Trypanosoma cruzi and Acanthamoeba castellanii str. Neff. The bioguided fractionation of the CHCl3 extract from the aerial part of P. inuloides leads to the isolation and characterization of quercetagetin-3,5,7,3'-tetramethylether as the active ingredient. Two acetylated derivatives were prepared from this natural compound and these three compounds were evaluated for their activities against the promastigote form of L. amazonensis. All these compounds exhibited moderate leishmanicidal activity with IC50 values ranging from 0.234 to 0.484 mM and low toxicity to macrophage cells (CC50 ranging from 0.365 to 0.664 mM). This study reported the antiprotozoal evaluation of Pulicaria inuloides for the first time and the results show that this species can be considered as a source of anti-leishmanicidal agents. The bioguided fractionation of the active extract of CHCl3 from C. albidus against T. cruzi led to the isolation of two fractions F6,4 and F6,5 which showed also a potent activity up to 100 μg/ml. The bioguided fractionation of the active extract of AcOEt from the aerial part of C. albidus against A. castellanii led to the isolation of a fraction F14A which showed a significant activity up to 100 μg / ml. Fractions F6,4 ; F6,5 and F14A consists of product mixtures, which have not been separated. We have also described the chemical compositions of the essential oils of Pulicaria inuloides and Cistus albidus. The major compounds of the species C. albidus are manool and 15,16-dinorlabd-8(20)- en-13-one whose skeleton of type labdane is a specific marker in this genus, these compounds are not described in samples from other regions and in particular in the Mediterranean regions (Spain and France) that appeared in the literature. The major compounds of the species Pulicaria inuloides are: δ- cadinene, α-muurolene, γ-cadinene, α-epi-cadinol and α-cadinol are not present in the other samples of Pulicaria inuloides from other areas published in the literature. In this study, the mineral content (inorganic elements) of 21 isolated extracts of various aromatic species of the Sahara (P. inuloides) and the Aures region (Euphorbia helioscopia L., Peganum harmala L., Daphne gnidium L., Calendula algeriensis L., Bunium incrassatum L., Echinops ritro L. Marrubium deserti de Noè., Juniperus oxycedrus L., Juniperus phoenicea L., Marrubium vulgare L., Cedrus atlantica (Endl.) Manetti and Thymus algeriensis L.) were also determined by inductively coupled plasma atomic emission spectroscopy (ICP-AES) and inductively coupled plasma mass spectroscopy (ICP-MS) . The results obtained showed higher concentrations of Ca, K, Mg, Na and S (mg/kg) in the different plant extracts. Diplôme : Doctorat En ligne : ../theses/chimie/FAD7287.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10902

Exemplaires (1)

Code-barres	Cote	Support	Localisation	Section	Disponibilité
FAD/7287	FAD/7287	Thèse	Bibliothèque principale	Thèses	Disponible

Préparation et évaluation biologique de composés polycycliques hybrides quinoléine-hétérocycles à visée thérapeutique / Hasna Haiour  

Public ISBD Titre : Préparation et évaluation biologique de composés polycycliques hybrides quinoléine-hétérocycles à visée thérapeutique Type de document : texte imprimé Auteurs : Hasna Haiour, Auteur ; Ali Belfaitah, Directeur de thèse Editeur : Constantine : Université Mentouri Constantine Année de publication : 2015 Importance : 182 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : Quinoléine  réaction d’addition-hétéro-cyclisation  hybride quinoléine-hétérocycle  Maladie ’Alzheimer  Tacrine  activité biologique  "Quinoline, addition-heterocyclisation reaction  poly-heterocyclic compounds  Alzheimer's disease  Tacrine’s analog  biological activity  ???????  ??????? ???????  ?????? ????????? ??? ??????? ??? ????????  ??? ????????  ??????  ?????? ???????? Index. décimale : 540 Chimie et sciences connexes Résumé : A number of original hybrids as (2-chloroquinolin-3-yl)-heterocyclic compounds were prepared from differently substituted 2-chloroquinolin-3-carbaldehydes. A series of4H-pyrans derivatives carriers an ester or ketone (aliphatic and cyclic), a nitrile and an amine functions linked in position 4 with variously substituted(2-chloroquinolin-3-yl) patterns (4a-4i) were prepared in very good yields (82-92%). Two series of (2-chloroquinolin-3-yl)-pyridine hybrids such as 2-amino-4-(2-chloroquinolin-3-yl)-6-substituted-nicotinonitriles (compounds 13-20), and 2-amino-4-(2-chloroquinolin-3-yl)-5,6,7,8-tetrahydroquinolin-3-carbonitrile derivatives (21-24) were prepared in variable yields (24-46%) from 3-(2-chloro-quinolin-3- yl)-2-cyanoacrylonitriles (3a-3d) as key intermediates in moderate yields (43-47%). The same approach was used to access to new highly functionalized (quinolin-6-yl)- heterocycles with various structures such as (quinolin-6-yl)-4H-pyran (32a-b, 33a et 34a-b), - 2-aminobenzochromene (35 et 36), and -1,4-dihydropyridine (compound 37), and that from a single intermediate the ethyl 2-chloro-6-formylquinolin-3-carboxylate (30). Yields are relatively low (10-20%) to acceptable (41-58%). A ""recovery"" hybrid derivatives (quinoline-3-yl)-4H-pyran was undertaken and resulted in the preparation of some series of highly original and diversely functionalized structural analogues of Tacrine (a bioactive compound used in the treatment of Alzheimer's disease). These pyranotacrines (quinolin-3-yl)-4H-pyran-tacrine) carriers in position 5 of 4H-pyran ring an electron-withdrawing group (series 5, 6, 7, 8; and compounds 9-12) were prepared under the standard conditions of the Friedländer’s reaction in satisfactory yields for most (39- 70%). The same conditions apply to (2-chloroquinolin-3-yl)-pyridine derivatives (13-20) do not appear altered these substrates (no evolution of the reaction). The in vitro biological evaluation (anti-Alzheimer's tests) of products of series 5,6,7, and compounds 9-12 as the determination of hepatotoxicity, measurement of inhibitory power toward acetylcholinesterase, butyrylcholinesterase, and induced aggregation of -amyloïd A1-40, neuroprotection and neurotoxicity, have shown that these new pyranotacrines are multipotent, non-hepatotoxic, non competitive acetylcholinesterase inhibitors, A1-40 antiaggregants, neuroprotective, and non-neurotoxic agents for Alzheimer’s disease. All prepared compounds were identified by usual spectroscopic methods (IR, 1H NMR and13C), and for some of them additional analyzes were carried out (X-ray diffraction, elemental analysis, MS and/or HRMS). Diplôme : Doctorat En ligne : ../theses/chimie/HAI6748.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=9867 Préparation et évaluation biologique de composés polycycliques hybrides quinoléine-hétérocycles à visée thérapeutique [texte imprimé] / Hasna Haiour, Auteur ; Ali Belfaitah, Directeur de thèse . - Constantine : Université Mentouri Constantine, 2015 . - 182 f. ; 30 cm. 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : Quinoléine  réaction d’addition-hétéro-cyclisation  hybride quinoléine-hétérocycle  Maladie ’Alzheimer  Tacrine  activité biologique  "Quinoline, addition-heterocyclisation reaction  poly-heterocyclic compounds  Alzheimer's disease  Tacrine’s analog  biological activity  ???????  ??????? ???????  ?????? ????????? ??? ??????? ??? ????????  ??? ????????  ??????  ?????? ???????? Index. décimale : 540 Chimie et sciences connexes Résumé : A number of original hybrids as (2-chloroquinolin-3-yl)-heterocyclic compounds were prepared from differently substituted 2-chloroquinolin-3-carbaldehydes. A series of4H-pyrans derivatives carriers an ester or ketone (aliphatic and cyclic), a nitrile and an amine functions linked in position 4 with variously substituted(2-chloroquinolin-3-yl) patterns (4a-4i) were prepared in very good yields (82-92%). Two series of (2-chloroquinolin-3-yl)-pyridine hybrids such as 2-amino-4-(2-chloroquinolin-3-yl)-6-substituted-nicotinonitriles (compounds 13-20), and 2-amino-4-(2-chloroquinolin-3-yl)-5,6,7,8-tetrahydroquinolin-3-carbonitrile derivatives (21-24) were prepared in variable yields (24-46%) from 3-(2-chloro-quinolin-3- yl)-2-cyanoacrylonitriles (3a-3d) as key intermediates in moderate yields (43-47%). The same approach was used to access to new highly functionalized (quinolin-6-yl)- heterocycles with various structures such as (quinolin-6-yl)-4H-pyran (32a-b, 33a et 34a-b), - 2-aminobenzochromene (35 et 36), and -1,4-dihydropyridine (compound 37), and that from a single intermediate the ethyl 2-chloro-6-formylquinolin-3-carboxylate (30). Yields are relatively low (10-20%) to acceptable (41-58%). A ""recovery"" hybrid derivatives (quinoline-3-yl)-4H-pyran was undertaken and resulted in the preparation of some series of highly original and diversely functionalized structural analogues of Tacrine (a bioactive compound used in the treatment of Alzheimer's disease). These pyranotacrines (quinolin-3-yl)-4H-pyran-tacrine) carriers in position 5 of 4H-pyran ring an electron-withdrawing group (series 5, 6, 7, 8; and compounds 9-12) were prepared under the standard conditions of the Friedländer’s reaction in satisfactory yields for most (39- 70%). The same conditions apply to (2-chloroquinolin-3-yl)-pyridine derivatives (13-20) do not appear altered these substrates (no evolution of the reaction). The in vitro biological evaluation (anti-Alzheimer's tests) of products of series 5,6,7, and compounds 9-12 as the determination of hepatotoxicity, measurement of inhibitory power toward acetylcholinesterase, butyrylcholinesterase, and induced aggregation of -amyloïd A1-40, neuroprotection and neurotoxicity, have shown that these new pyranotacrines are multipotent, non-hepatotoxic, non competitive acetylcholinesterase inhibitors, A1-40 antiaggregants, neuroprotective, and non-neurotoxic agents for Alzheimer’s disease. All prepared compounds were identified by usual spectroscopic methods (IR, 1H NMR and13C), and for some of them additional analyzes were carried out (X-ray diffraction, elemental analysis, MS and/or HRMS). Diplôme : Doctorat En ligne : ../theses/chimie/HAI6748.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=9867

Exemplaires (1)

Code-barres	Cote	Support	Localisation	Section	Disponibilité
HAI/6748	HAI/6748	Thèse	Bibliothèque principale	Thèses	Disponible

Synthese et reactivite de derivies de laquinoleique / Saida Benzerka    

Public ISBD Titre : Synthese et reactivite de derivies de laquinoleique : Preparation de composes polycycliques a visee therapeutique Type de document : texte imprimé Auteurs : Saida Benzerka, Auteur ; Ali Belfaitah, Directeur de thèse Editeur : constantine [Algérie] : Université Constantine 1 Année de publication : 2014 Importance : 173 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : 2-phenylquinoléine  fonctionnalisation  activité biologique  aza-coumarine  naphthydrine  ylure d’azométhine  polycyles  2-phenylquinoline  functionalization  biological activity  aza-coumarin  naphthydrin  azomethine ylide  polycyclic compounds  2- ???? ???????  ???????? ??????????  ?????? ????? Index. décimale : 540 Chimie et sciences connexes Résumé : A number of polycyclic compounds containing a quinoline entity as a basic structural core were prepared using appropriate synthetic routes. In this work, a single base material was used: the 2-chloro-3-formyl-6-methylquinoline. Three series of compound derived from 2-phenylquinoline bearing at the position 3 respectively an amide function, ester and amine, linked to various groups such as a straight or branched chain alkyl having varying lengths, a five or six membered saturated cycle, and other aromatics, have been synthesized. The incorporation of an amine group in position 5 of the quinoline nucleus, and the functionalization of the aromatic methyl in position 6, has also been explored. The bromination reaction of the aromatic methyl with NBS provides selectively the mono or dibrominated derivative. The addition of morpholine to the monobrominated compound affords the corresponding amine, while the oxidation of ethyl 6-(dibromethyl)-2-chloroquinoléin-3-carboxylate by AgNO3 generates the aldehyde function. Several approaches using various reactions such as substitution reaction, addition- elimination (aldolization), cycloaddition, oxidation, reduction and other related synthesis methods have been developed for the preparation of 3-heteroaryl-2-phénylquinoléines. Some 2-phenylquinoline derivatives bearing at position 3, a pyrazole, pyrrole, oxazole, oxazolone, coumarin or quinoline, were prepared in good yields. The antimicrobial activity evaluation of prepared compounds, belonging to each of two themes, was carried out on five approved bacterial strains (Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae and Salmonella thipymurium) using two different methods: the disk-diffusion, and the determination of minimum inhibitory concentration (MIC). The analysis of the results shows that most of the tested compounds are active against selected strains and some of them possess a remarkable bactericidal power (MIC ≤ 50 g / mL). The synthesis of condensed poly-heterocycles was undertaken and resulted in the preparation of few compounds derived from aza-coumarin analogs (benzo[6,7]-8-azacoumarins), and naphthydrin (benzo[6,7]-1,8-naphthydrins). The reactivity of 12-methyl-benzo[6,7]-8-azacoumarin and benzo[6,7]-1,12-dimethyl-1,2-dihydro-1,8-naphthydrin-3-carbonitrile through the 1,3-dipolar cycloaddition reaction of non-stabilized azomethine ylide, which is generated in situ by thermal decarboxylation of N-methyl-5-oxazolidinone, has also been explored. No reaction took place for the first one, but the second dipolarophile reacts correctly giving the condensed tetracyclic adduct, as expected. Yields are good, and structures of all prepared compounds were elucidated by usual spectroscopic methods (IR, NMR1H and C-13, and single-crystal-X-Ray diffraction). Diplôme : Doctorat en sciences En ligne : ../theses/chimie/BEN6486.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=9535 Synthese et reactivite de derivies de laquinoleique : Preparation de composes polycycliques a visee therapeutique [texte imprimé] / Saida Benzerka, Auteur ; Ali Belfaitah, Directeur de thèse . - constantine (Route ain el bey, Algérie) : Université Constantine 1, 2014 . - 173 f. ; 30 cm. 2 copies imprimées disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : 2-phenylquinoléine  fonctionnalisation  activité biologique  aza-coumarine  naphthydrine  ylure d’azométhine  polycyles  2-phenylquinoline  functionalization  biological activity  aza-coumarin  naphthydrin  azomethine ylide  polycyclic compounds  2- ???? ???????  ???????? ??????????  ?????? ????? Index. décimale : 540 Chimie et sciences connexes Résumé : A number of polycyclic compounds containing a quinoline entity as a basic structural core were prepared using appropriate synthetic routes. In this work, a single base material was used: the 2-chloro-3-formyl-6-methylquinoline. Three series of compound derived from 2-phenylquinoline bearing at the position 3 respectively an amide function, ester and amine, linked to various groups such as a straight or branched chain alkyl having varying lengths, a five or six membered saturated cycle, and other aromatics, have been synthesized. The incorporation of an amine group in position 5 of the quinoline nucleus, and the functionalization of the aromatic methyl in position 6, has also been explored. The bromination reaction of the aromatic methyl with NBS provides selectively the mono or dibrominated derivative. The addition of morpholine to the monobrominated compound affords the corresponding amine, while the oxidation of ethyl 6-(dibromethyl)-2-chloroquinoléin-3-carboxylate by AgNO3 generates the aldehyde function. Several approaches using various reactions such as substitution reaction, addition- elimination (aldolization), cycloaddition, oxidation, reduction and other related synthesis methods have been developed for the preparation of 3-heteroaryl-2-phénylquinoléines. Some 2-phenylquinoline derivatives bearing at position 3, a pyrazole, pyrrole, oxazole, oxazolone, coumarin or quinoline, were prepared in good yields. The antimicrobial activity evaluation of prepared compounds, belonging to each of two themes, was carried out on five approved bacterial strains (Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae and Salmonella thipymurium) using two different methods: the disk-diffusion, and the determination of minimum inhibitory concentration (MIC). The analysis of the results shows that most of the tested compounds are active against selected strains and some of them possess a remarkable bactericidal power (MIC ≤ 50 g / mL). The synthesis of condensed poly-heterocycles was undertaken and resulted in the preparation of few compounds derived from aza-coumarin analogs (benzo[6,7]-8-azacoumarins), and naphthydrin (benzo[6,7]-1,8-naphthydrins). The reactivity of 12-methyl-benzo[6,7]-8-azacoumarin and benzo[6,7]-1,12-dimethyl-1,2-dihydro-1,8-naphthydrin-3-carbonitrile through the 1,3-dipolar cycloaddition reaction of non-stabilized azomethine ylide, which is generated in situ by thermal decarboxylation of N-methyl-5-oxazolidinone, has also been explored. No reaction took place for the first one, but the second dipolarophile reacts correctly giving the condensed tetracyclic adduct, as expected. Yields are good, and structures of all prepared compounds were elucidated by usual spectroscopic methods (IR, NMR1H and C-13, and single-crystal-X-Ray diffraction). Diplôme : Doctorat en sciences En ligne : ../theses/chimie/BEN6486.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=9535

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Synthèse, caractérisation et évaluation biologique de nouveaux dérivés poly-hétérocycliques à base d’imidazole / Houssem Boulebd  

Public ISBD Titre : Synthèse, caractérisation et évaluation biologique de nouveaux dérivés poly-hétérocycliques à base d’imidazole Type de document : texte imprimé Auteurs : Houssem Boulebd, Auteur ; Ali Belfaitah, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2016 Importance : 257 f. Format : 30 cm. Note générale : 2 copies imprimes disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : Chimie organique  Imidazole  halogénation  poly-hétérocycles  Maladie d’Alzheimer  analogues de la Tacrine  hépatotoxicité  ORAC  activité biologique  ?????????  ?????  ????? ??????? ????? ???????  ??? ????????  ?????????????  ????  ORAC?????? ???????? Imidazole  halogenation  poly-heterocyclic compounds  Alzheimer's disease tacrine analogues  hepatotoxicity  biological activity Index. décimale : 540 Chimie et sciences connexes Résumé : Some 2-halo-(1-methyl-1H-imidazole) derivatives were prepared by selective halogenation reaction (bromination, chlorination and iodination). The addition of -bromoacetophenone to 2-bromo(chloro)-1-methyl-1H-imidazole allowed us to access to corresponding imidazolium salts in satisfactory yields (47-64%). The reactivity of 2-halogeno-N-phenyl-1-methyl-1Himidazolium bromide with activated methylene compounds of diverse structures has been studied. A series of original heterocyclic products composed of a core 1-methyl-1H-imidazole associated at 2-position to highly functionalized heterocyclic compounds such as 4H-pyran, chromene, benzo (pyrido) chromenes, 1,4-dihydropyridine, pyridine, quinazoline, pyrrolidines and other pyrazolines have been prepared. It will be noted that upon addition of methyl ketone derivatives, 1-methylimidazole-pyridine hybrid compounds obtained are accompanied by the formation of corresponding 2,6- dicyanoaniline derivatives in low yields. The adaptation of the operating conditions enabled us to selectively direct the reaction towards the formation of new 2,6-dicyanoaniline derivatives in good yields for aliphatic methyl ketone derivatives (62-70%), and in 45 % of yield for acetophenone. These compounds are also fluorescent. Some series of hybrid compounds such as (1-methyl-1H-imidazol-2-yl)-4H-pyran, - pyridine, -1,4-dihydropyridine and -quinazoline have been subjected to an in vitro assessment of their antimicrobial, and antioxydante (DPPH) activities, and also for their hepatotoxicity towards liver cells HepG2 in a gradient concentration from 1M to 300M, and a structureactivity relationship (SAR) has been demonstrated. A "valorization" of (1-methyl-1H-imidazol-2-yl)-4-pyran hybrid derivatives was undertaken and resulted in the preparation of some original series of highly and diversely functionalized Tacrine analogues (Tacrine is a drug used in the treatment of Alzheimer's disease) as pyranotacrines. These novel racemic Tacrine analogues are siginificantly less hepatotoxic than Tacrine, retaining potent, and selective EeAChE inhibition with IC50 values in the M range, with a remarkable antioxydant effect. Yields are good in most cases. All prepared compounds were identified by the usual spectroscopic methods (IR, 1H NMR and 13C NMR), and for some of them additional analyzes were carried out (elemental analysis and / or X-ray diffraction). Diplôme : Doctorat En ligne : ../theses/chimie/BOU6833.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10125 Synthèse, caractérisation et évaluation biologique de nouveaux dérivés poly-hétérocycliques à base d’imidazole [texte imprimé] / Houssem Boulebd, Auteur ; Ali Belfaitah, Directeur de thèse . - [S.l.] : جامعة الإخوة منتوري قسنطينة, 2016 . - 257 f. ; 30 cm. 2 copies imprimes disponibles Langues : Français (fre) Catégories : Français - Anglais Chimie Tags : Chimie organique  Imidazole  halogénation  poly-hétérocycles  Maladie d’Alzheimer  analogues de la Tacrine  hépatotoxicité  ORAC  activité biologique  ?????????  ?????  ????? ??????? ????? ???????  ??? ????????  ?????????????  ????  ORAC?????? ???????? Imidazole  halogenation  poly-heterocyclic compounds  Alzheimer's disease tacrine analogues  hepatotoxicity  biological activity Index. décimale : 540 Chimie et sciences connexes Résumé : Some 2-halo-(1-methyl-1H-imidazole) derivatives were prepared by selective halogenation reaction (bromination, chlorination and iodination). The addition of -bromoacetophenone to 2-bromo(chloro)-1-methyl-1H-imidazole allowed us to access to corresponding imidazolium salts in satisfactory yields (47-64%). The reactivity of 2-halogeno-N-phenyl-1-methyl-1Himidazolium bromide with activated methylene compounds of diverse structures has been studied. A series of original heterocyclic products composed of a core 1-methyl-1H-imidazole associated at 2-position to highly functionalized heterocyclic compounds such as 4H-pyran, chromene, benzo (pyrido) chromenes, 1,4-dihydropyridine, pyridine, quinazoline, pyrrolidines and other pyrazolines have been prepared. It will be noted that upon addition of methyl ketone derivatives, 1-methylimidazole-pyridine hybrid compounds obtained are accompanied by the formation of corresponding 2,6- dicyanoaniline derivatives in low yields. The adaptation of the operating conditions enabled us to selectively direct the reaction towards the formation of new 2,6-dicyanoaniline derivatives in good yields for aliphatic methyl ketone derivatives (62-70%), and in 45 % of yield for acetophenone. These compounds are also fluorescent. Some series of hybrid compounds such as (1-methyl-1H-imidazol-2-yl)-4H-pyran, - pyridine, -1,4-dihydropyridine and -quinazoline have been subjected to an in vitro assessment of their antimicrobial, and antioxydante (DPPH) activities, and also for their hepatotoxicity towards liver cells HepG2 in a gradient concentration from 1M to 300M, and a structureactivity relationship (SAR) has been demonstrated. A "valorization" of (1-methyl-1H-imidazol-2-yl)-4-pyran hybrid derivatives was undertaken and resulted in the preparation of some original series of highly and diversely functionalized Tacrine analogues (Tacrine is a drug used in the treatment of Alzheimer's disease) as pyranotacrines. These novel racemic Tacrine analogues are siginificantly less hepatotoxic than Tacrine, retaining potent, and selective EeAChE inhibition with IC50 values in the M range, with a remarkable antioxydant effect. Yields are good in most cases. All prepared compounds were identified by the usual spectroscopic methods (IR, 1H NMR and 13C NMR), and for some of them additional analyzes were carried out (elemental analysis and / or X-ray diffraction). Diplôme : Doctorat En ligne : ../theses/chimie/BOU6833.pdf Format de la ressource électronique : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10125

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