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Partager le résultat de cette recherche Interroger des sources externesSynthèse, caractérisation et évaluation biologique de nouveaux dérivés poly-hétérocycliques à base d’imidazole / Houssem Boulebd
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
ChimieTags : Chimie organique Imidazole halogénation poly-hétérocycles Maladie d’Alzheimer analogues de la
Tacrine hépatotoxicité ORAC activité biologique إيميدازول هلجنة متعدد الحلقات الغير متجانسة مرض الزهايمر نظائرالتاكرين سمية ORACفعالية بيولوجية
Imidazole halogenation poly-heterocyclic compounds Alzheimer's disease
tacrine analogues hepatotoxicity biological activityIndex. 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 1M to 300M, 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 : Permalink : 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 . - جامعة الإخوة منتوري قسنطينة, 2016 . - 257 f. ; 30 cm.
2 copies imprimes disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : Chimie organique Imidazole halogénation poly-hétérocycles Maladie d’Alzheimer analogues de la
Tacrine hépatotoxicité ORAC activité biologique إيميدازول هلجنة متعدد الحلقات الغير متجانسة مرض الزهايمر نظائرالتاكرين سمية ORACفعالية بيولوجية
Imidazole halogenation poly-heterocyclic compounds Alzheimer's disease
tacrine analogues hepatotoxicity biological activityIndex. 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 1M to 300M, 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 : Permalink : index.php?lvl=notice_display&id=10125 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité BOU/6833 BOU/6833 Thèse Bibliothèque principale Thèses Disponible
Titre : Conception et synthèse en série hétérocyclique de nouveaux dérivés quinazolinoquinoléines et pyrimidines polyfonctionalisés à intérêt biologique potentiel. Type de document : texte imprimé Auteurs : Imen Boualia, Auteur ; Raouf Boulcina, Directeur de thèse Mention d'édition : 18/11/2019 Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2019 Importance : 240 f. Format : 30 cm. Note générale : Doctorat 3éme CYCLE LMD.
1 copies imprimées disponibles
Langues : Français (fre) Catégories : Français - Anglais
ChimieTags : Chimie: chimie organique "Dihydroquinazolinones quinazolinones poly-hétérocycles condensation de Knoevenagel quinazolino-quinoléines pyrimidines Maladie d’Alzheimer activité biologique Knoevenagel condensation Alzheimer's disease biological activity ديهيدروكوينازولينون كينازولينون متعدد الحلقات تكاثف كينوزولينو كينولين بيريميدين مرض
الزهايمر فعالية بيولوجيةIndex. décimale : 540 Chimie et sciences connexes Résumé :
In this manuscript, we are interested in research focused on the synthesis of new biologically active heterocyclic compounds. This thesis consists of two main parts: The first part was dedicated to the preparation of the new original quinazoline-quinoléine hybrid heterocyclic derivatives and the functionalization of the 4 and 2' positions of 4-chloroquinazoline-2'-chloroquinoléine derivatives, which have interesting biological properties. The present method doesn’t require the use of expensive catalysts or complex ligands and can be considered a useful alternative to Suzuki reaction, even if it was limited to electron-rich partners. In the second part of this work, we report the development of a new synthetic pathway for the preparation of a rich and wide library of substituted 4-amino-5-cyano-pyrimidines and bis(4- amino-5-cyano-pyrimidines), using the K2CO3 as catalysts. The obtained molecules possess a good biological interest (anti-cholinesterase, antioxidant and antimicrobials).
Note de contenu : Annexes. Diplôme : Doctorat En ligne : ../theses/chimie/BOU7578.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11416 Conception et synthèse en série hétérocyclique de nouveaux dérivés quinazolinoquinoléines et pyrimidines polyfonctionalisés à intérêt biologique potentiel. [texte imprimé] / Imen Boualia, Auteur ; Raouf Boulcina, Directeur de thèse . - 18/11/2019 . - جامعة الإخوة منتوري قسنطينة, 2019 . - 240 f. ; 30 cm.
Doctorat 3éme CYCLE LMD.
1 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : Chimie: chimie organique "Dihydroquinazolinones quinazolinones poly-hétérocycles condensation de Knoevenagel quinazolino-quinoléines pyrimidines Maladie d’Alzheimer activité biologique Knoevenagel condensation Alzheimer's disease biological activity ديهيدروكوينازولينون كينازولينون متعدد الحلقات تكاثف كينوزولينو كينولين بيريميدين مرض
الزهايمر فعالية بيولوجيةIndex. décimale : 540 Chimie et sciences connexes Résumé :
In this manuscript, we are interested in research focused on the synthesis of new biologically active heterocyclic compounds. This thesis consists of two main parts: The first part was dedicated to the preparation of the new original quinazoline-quinoléine hybrid heterocyclic derivatives and the functionalization of the 4 and 2' positions of 4-chloroquinazoline-2'-chloroquinoléine derivatives, which have interesting biological properties. The present method doesn’t require the use of expensive catalysts or complex ligands and can be considered a useful alternative to Suzuki reaction, even if it was limited to electron-rich partners. In the second part of this work, we report the development of a new synthetic pathway for the preparation of a rich and wide library of substituted 4-amino-5-cyano-pyrimidines and bis(4- amino-5-cyano-pyrimidines), using the K2CO3 as catalysts. The obtained molecules possess a good biological interest (anti-cholinesterase, antioxidant and antimicrobials).
Note de contenu : Annexes. Diplôme : Doctorat En ligne : ../theses/chimie/BOU7578.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11416 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité BOU/7578 BOU/7578 Thèse Bibliothèque principale Thèses Disponible
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) Catégories : Français - Anglais
ChimieTags : 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 إيميدازول بنزيميدازول المعقدات المعادن الانتقالية ثنائية التكافؤ النشاط المضاد للأكسدة التاكرين البنزوبرانوتاكرين النشاط المضاد للميكروبات 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 : 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 . - جامعة الإخوة منتوري قسنطينة, 2018 . - 186 f. ; 30 cm.
2 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : 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 إيميدازول بنزيميدازول المعقدات المعادن الانتقالية ثنائية التكافؤ النشاط المضاد للأكسدة التاكرين البنزوبرانوتاكرين النشاط المضاد للميكروبات 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 : index.php?lvl=notice_display&id=11008 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité LIF/7359 LIF/7359 Thèse Bibliothèque principale Thèses Disponible
