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Partager le résultat de cette recherche Interroger des sources externesPréparation de nouveaux matériaux à base de (benz)imidazole et bio-activité / Anfel Benhassine ép Lifa
Titre : Préparation de nouveaux matériaux à base de (benz)imidazole et bio-activité : synthèse de complexes à base de (benz)imidazole, étude structurale et théorique et préparation d’analogues structuraux de la Tacrine à base de benzimidazole. Type de document : texte imprimé Auteurs : Anfel Benhassine ép Lifa, Auteur ; Ali Belfaitah, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2018 Importance : 186 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles
Langues : Français (fre) Tags : Imidazole Benzimidazole Complexassion Métaux de transition divalents DFT orbitales frontières Tacrine réaction de Friedländer poly-hétérocycles DPPH ABTS activité antimicrobienne Divalent transition metals calculations Frontier orbitals Friedländer's reaction poly-heterocyclic compounds antimicrobial activity ????????? ??????????? ???????? ??????? ?????????? ?????? ??????? ?????? ?????? ??????? ???????? ????????????????? ?????? ?????? ?????????? Index. décimale : 540 Chimie et sciences connexes Résumé : The first part, which is subdivided into two chapters, concerns the synthesis, characterization (IR and UV-Vis, X-ray diffraction, and other elemental analysis) and biological evaluation of divalent transition metal complexes (M = Co , Cu, Cd, Zn, Ni) based on (1-methyl- 1Hbenzo[d]imidazol-2-yl) methanol (L1/Hmbm) (complexes 1-4) and (1-methyl-1H- imidazol-2-yl) methanol (L2/Hmim) (complexes 5-11). In both series of coordination compounds, the ligand (L1 or L2) gives rise to a variety of metal-ligand coordination modes(monodentate or bidentadate) exhibiting tetrahedral or octahedral geometry.The in vitro measurement of the antioxidant activity of the L1 and L2 ligands and their respective metal complexes against the free radical scavenger DPPH at low concentration (100 &g / mL), showed a moderate to significant antioxidant activities, compared to the standard (Asc). The complexes (5-11) and the ligand L2 were submitted to an in vitro evaluation of their antimicrobial activity against five pathogenic strains: animal bacteria:
Gram (+) (S. aureus) and Gram (-) (K pneumonia), a Gram (+) phytopathogenic bacterium (P.
syringae), a yeast (P. caribbica) and a fungus (Trichodermsp), using the disk diffusion method
(agar).The analysis of the results revealed a significant difference in the inhibition profile of the selected strains. The complex 5 and to a lesser extent the complex 6, gave the best results displaying significant inhibitory activities on mostly all pathogenic strains (broad spectrum). In the second part dedicated to the synthesis of structural analogs of Tacrine, a whole series of new poly-heterocyclic compounds (10-14) was prepared from the corresponding 4H-pyrans (5- 9) by an addition-hetero-cyclization reaction of cyclohexanone under the Friedl‰ndler's standard conditions reaction. The in vitro antioxidant tests (DPPH and ABTS) of
benzimidazopyranotacrines, showed that the five compounds have an antioxidant activities, and
the 5-Amino-2-methyl-4-(1-methyl-1H-benzo[d]imidazol-2-yl)-6,7,8,9-tetrahydro-4H-pyrano
[2,3-b]uinolin-3-yl) ethanone (compound 12) is the most efficient, exhibiting a comparable
inhibitory power of free radicals to that of reference compounds (controls). The structure of all the complexes (1-11) was determined by X-ray diffraction, IR, UV and other elemental analysis. For complexes 1-4, theoretical studies using DFT and TD-DFT calculations have been performed and confirmed the experimental results. Benzimidazopyranotacrines (10-14) as structural Tacrine's analogues and their intermediates 4Hpyrans (5-9), were identified by the usual spectroscopic methods (IR, 1H NMR and13C).Diplôme : Doctorat En ligne : ../theses/chimie/LIF7359.pdf Format de la ressource électronique : Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=11008 Préparation de nouveaux matériaux à base de (benz)imidazole et bio-activité : synthèse de complexes à base de (benz)imidazole, étude structurale et théorique et préparation d’analogues structuraux de la Tacrine à base de benzimidazole. [texte imprimé] / Anfel Benhassine ép Lifa, Auteur ; Ali Belfaitah, Directeur de thèse . - [S.l.] : جامعة الإخوة منتوري قسنطينة, 2018 . - 186 f. ; 30 cm.
2 copies imprimées disponibles
Langues : Français (fre)
Tags : Imidazole Benzimidazole Complexassion Métaux de transition divalents DFT orbitales frontières Tacrine réaction de Friedländer poly-hétérocycles DPPH ABTS activité antimicrobienne Divalent transition metals calculations Frontier orbitals Friedländer's reaction poly-heterocyclic compounds antimicrobial activity ????????? ??????????? ???????? ??????? ?????????? ?????? ??????? ?????? ?????? ??????? ???????? ????????????????? ?????? ?????? ?????????? Index. décimale : 540 Chimie et sciences connexes Résumé : The first part, which is subdivided into two chapters, concerns the synthesis, characterization (IR and UV-Vis, X-ray diffraction, and other elemental analysis) and biological evaluation of divalent transition metal complexes (M = Co , Cu, Cd, Zn, Ni) based on (1-methyl- 1Hbenzo[d]imidazol-2-yl) methanol (L1/Hmbm) (complexes 1-4) and (1-methyl-1H- imidazol-2-yl) methanol (L2/Hmim) (complexes 5-11). In both series of coordination compounds, the ligand (L1 or L2) gives rise to a variety of metal-ligand coordination modes(monodentate or bidentadate) exhibiting tetrahedral or octahedral geometry.The in vitro measurement of the antioxidant activity of the L1 and L2 ligands and their respective metal complexes against the free radical scavenger DPPH at low concentration (100 &g / mL), showed a moderate to significant antioxidant activities, compared to the standard (Asc). The complexes (5-11) and the ligand L2 were submitted to an in vitro evaluation of their antimicrobial activity against five pathogenic strains: animal bacteria:
Gram (+) (S. aureus) and Gram (-) (K pneumonia), a Gram (+) phytopathogenic bacterium (P.
syringae), a yeast (P. caribbica) and a fungus (Trichodermsp), using the disk diffusion method
(agar).The analysis of the results revealed a significant difference in the inhibition profile of the selected strains. The complex 5 and to a lesser extent the complex 6, gave the best results displaying significant inhibitory activities on mostly all pathogenic strains (broad spectrum). In the second part dedicated to the synthesis of structural analogs of Tacrine, a whole series of new poly-heterocyclic compounds (10-14) was prepared from the corresponding 4H-pyrans (5- 9) by an addition-hetero-cyclization reaction of cyclohexanone under the Friedl‰ndler's standard conditions reaction. The in vitro antioxidant tests (DPPH and ABTS) of
benzimidazopyranotacrines, showed that the five compounds have an antioxidant activities, and
the 5-Amino-2-methyl-4-(1-methyl-1H-benzo[d]imidazol-2-yl)-6,7,8,9-tetrahydro-4H-pyrano
[2,3-b]uinolin-3-yl) ethanone (compound 12) is the most efficient, exhibiting a comparable
inhibitory power of free radicals to that of reference compounds (controls). The structure of all the complexes (1-11) was determined by X-ray diffraction, IR, UV and other elemental analysis. For complexes 1-4, theoretical studies using DFT and TD-DFT calculations have been performed and confirmed the experimental results. Benzimidazopyranotacrines (10-14) as structural Tacrine's analogues and their intermediates 4Hpyrans (5-9), were identified by the usual spectroscopic methods (IR, 1H NMR and13C).Diplôme : Doctorat En ligne : ../theses/chimie/LIF7359.pdf Format de la ressource électronique : Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=11008 Exemplaires
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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) 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 A1-40, neuroprotection and neurotoxicity, have shown that these new pyranotacrines are multipotent, non-hepatotoxic, non competitive acetylcholinesterase inhibitors, A1-40 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 : 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)
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 A1-40, neuroprotection and neurotoxicity, have shown that these new pyranotacrines are multipotent, non-hepatotoxic, non competitive acetylcholinesterase inhibitors, A1-40 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 : Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=9867 Exemplaires
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Titre : Synthèse et caractérisation de poly-hétérocycles bioactifs Type de document : texte imprimé Auteurs : Chamseddine Derabli, Auteur ; Raouf Boulcina, Directeur de thèse Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2016 Importance : 217 f. Format : 30 cm. Note générale : 2 copies imprimées disponibles
Langues : Français (fre) Tags : Quinolones cyclisation d’aza-Michael liquides ioniques quinazolines quinazolinones quinoléines pyranopyrazoles pyrimidines Tacrine Maladie d’Alzheimer aza-Michael cyclization ionic liquids quinolines Alzheimer's disease ??????????? ???? ???-??????? ?????? ??????? ????????????? ??????? ????????? ?????? ???
??????????Index. décimale : 540 Chimie et sciences connexes Résumé : This manuscript includes three main parts:
In the first chapter, we described a new method for preparation of 2-aryl-2,3-dihydro-4-quinolonesby the use of the cyclization of the corresponding 2-aminochalconesvia an azaMichael reaction. This method was catalyzed by a DABCO’s ionic liquid which allowed us to obtain quantitatively our intended products in a single step.
In the second chapter, we synthesized a series of new 1,2-dihydroquinazoline derivatives by a one pot reaction, from benzaldehyde derivatives, ammonium acetate and 2-aminobenzophenones in the presence of DMAP. Similarly, we described the synthesis of new hybrid quinazoline-quinoline compounds from raw materials and other easily accessible key intermediates.
Finally, the study that we have undertaken in this final chapter of the thesis has as main objective, the preparation of novel heterocyclic analogues of Tacrine (used in the treatment of Alzheimer's disease) based pyranopyrazole and pyrimidine structures.
Diplôme : Doctorat Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10221 Synthèse et caractérisation de poly-hétérocycles bioactifs [texte imprimé] / Chamseddine Derabli, Auteur ; Raouf Boulcina, Directeur de thèse . - [S.l.] : جامعة الإخوة منتوري قسنطينة, 2016 . - 217 f. ; 30 cm.
2 copies imprimées disponibles
Langues : Français (fre)
Tags : Quinolones cyclisation d’aza-Michael liquides ioniques quinazolines quinazolinones quinoléines pyranopyrazoles pyrimidines Tacrine Maladie d’Alzheimer aza-Michael cyclization ionic liquids quinolines Alzheimer's disease ??????????? ???? ???-??????? ?????? ??????? ????????????? ??????? ????????? ?????? ???
??????????Index. décimale : 540 Chimie et sciences connexes Résumé : This manuscript includes three main parts:
In the first chapter, we described a new method for preparation of 2-aryl-2,3-dihydro-4-quinolonesby the use of the cyclization of the corresponding 2-aminochalconesvia an azaMichael reaction. This method was catalyzed by a DABCO’s ionic liquid which allowed us to obtain quantitatively our intended products in a single step.
In the second chapter, we synthesized a series of new 1,2-dihydroquinazoline derivatives by a one pot reaction, from benzaldehyde derivatives, ammonium acetate and 2-aminobenzophenones in the presence of DMAP. Similarly, we described the synthesis of new hybrid quinazoline-quinoline compounds from raw materials and other easily accessible key intermediates.
Finally, the study that we have undertaken in this final chapter of the thesis has as main objective, the preparation of novel heterocyclic analogues of Tacrine (used in the treatment of Alzheimer's disease) based pyranopyrazole and pyrimidine structures.
Diplôme : Doctorat Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=10221 Exemplaires
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