2 résultat(s) recherche sur le tag 'poly-hétérocycles'    

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) 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) 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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Préparation de nouveaux matériaux à base de (benz)imidazole et bio-activité / Anfel Benhassine ép Lifa  

Public ISBD 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 : pdf 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 : pdf Permalink : https://bu.umc.edu.dz/md/index.php?lvl=notice_display&id=11008

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