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Partager le résultat de cette recherche Interroger des sources externesEtude de la tolerance au gluso,insuline,cortisol,homocysteine et determination du polymorphisme des genes APOE et MTHFR dans la maladie d'alzheimer / Ahmed Ouldjaoui
Titre : Etude de la tolerance au gluso,insuline,cortisol,homocysteine et determination du polymorphisme des genes APOE et MTHFR dans la maladie d'alzheimer : etude de population :Nord Constantinois Type de document : texte imprimé Auteurs : Ahmed Ouldjaoui, Auteur ; N. Abadi, Directeur de thèse Editeur : Constantine : Université Mentouri Constantine Année de publication : 2011 Importance : 184 f. Format : 31 cm. Note générale : Doctorat en sciences
2 copies imprimées disponibleLangues : Français (fre) Catégories : Français - Anglais
ChimieTags : ApoE polymorphisme maladie d’Alzheimer lipoprotéines cholestérol cortisol Index. décimale : 540 Chimie et sciences connexes Diplôme : Doctorat en sciences En ligne : ../theses/biologie/OUL6039.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=6224 Etude de la tolerance au gluso,insuline,cortisol,homocysteine et determination du polymorphisme des genes APOE et MTHFR dans la maladie d'alzheimer : etude de population :Nord Constantinois [texte imprimé] / Ahmed Ouldjaoui, Auteur ; N. Abadi, Directeur de thèse . - Constantine : Université Mentouri Constantine, 2011 . - 184 f. ; 31 cm.
Doctorat en sciences
2 copies imprimées disponible
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : ApoE polymorphisme maladie d’Alzheimer lipoprotéines cholestérol cortisol Index. décimale : 540 Chimie et sciences connexes Diplôme : Doctorat en sciences En ligne : ../theses/biologie/OUL6039.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=6224 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité OUL/6039 OUL/6039 Thèse Bibliothèque principale Thèses Disponible
Titre : Identification par criblage virtuel et analyses biologiques de nouveaux inhibiteurs de l’acétylcholinestérase pour le traitement de la maladie d’Alzheimer. Type de document : texte imprimé Auteurs : El-Hassen Mokrani, Auteur ; Abderrahmane Bensegueni, Directeur de thèse Mention d'édition : 18/10/2020 Editeur : جامعة الإخوة منتوري قسنطينة Année de publication : 2020 Importance : 169 f. Format : 30 cm. Note générale : 1 copies imprimées disponibles
Langues : Français (fre) Catégories : Français - Anglais
BiologieTags : Biochimie et Biologie Cellulaire et Moléculaire: Biochimie Appliquée Acétylcholinestérase Criblage virtuel Inhibiteur Maladie d’Alzheimer vSDC Alzheimer’s disease inhibitory activity Virtual screening أستيل كولينستراز مرض الزهايمر نشاط مثبط فحص افتراضي Index. décimale : 570 Sciences de la vie. Biologie Résumé :
Acetylcholinesterase (AChE) is currently the most favorable target for the symptomatic treatment and reduction of Alzheimer’s disease (AD). In this work, a new structure-based virtual screening strategy was used in order to identify, among 14307 compounds of Institut Curie-CNRS chemical library, new potent AChE inhibitors. The strategy undertaken in this work consisted of the use of several docking programs in SBVS calculations followed by the application of a consensus method (vSDC) and a scrupulous visual analysis. It allowed us to obtain a high degree of success, with a yield of almost 86%, since 12 hits were identified among only 14 molecules tested in vitro. Still more remarkably, 6 of these hits were more active than galantamine, the reference inhibitor. These hits were predicted to have good ADMET properties. Finally, the in vivo study of cytotoxicity undertaken on Artemia salina larvae showed, in particular, through the evaluation of the LC50 / IC50 ratio that the six hits have a greater inhibitory activity than their toxic effect, which can thus be used as starting structures for the optimization and design of new AD drug candidates.
Note de contenu :
Annexes.Diplôme : Doctorat en sciences En ligne : ../theses/biologie/MOK7666.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11500 Identification par criblage virtuel et analyses biologiques de nouveaux inhibiteurs de l’acétylcholinestérase pour le traitement de la maladie d’Alzheimer. [texte imprimé] / El-Hassen Mokrani, Auteur ; Abderrahmane Bensegueni, Directeur de thèse . - 18/10/2020 . - جامعة الإخوة منتوري قسنطينة, 2020 . - 169 f. ; 30 cm.
1 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
BiologieTags : Biochimie et Biologie Cellulaire et Moléculaire: Biochimie Appliquée Acétylcholinestérase Criblage virtuel Inhibiteur Maladie d’Alzheimer vSDC Alzheimer’s disease inhibitory activity Virtual screening أستيل كولينستراز مرض الزهايمر نشاط مثبط فحص افتراضي Index. décimale : 570 Sciences de la vie. Biologie Résumé :
Acetylcholinesterase (AChE) is currently the most favorable target for the symptomatic treatment and reduction of Alzheimer’s disease (AD). In this work, a new structure-based virtual screening strategy was used in order to identify, among 14307 compounds of Institut Curie-CNRS chemical library, new potent AChE inhibitors. The strategy undertaken in this work consisted of the use of several docking programs in SBVS calculations followed by the application of a consensus method (vSDC) and a scrupulous visual analysis. It allowed us to obtain a high degree of success, with a yield of almost 86%, since 12 hits were identified among only 14 molecules tested in vitro. Still more remarkably, 6 of these hits were more active than galantamine, the reference inhibitor. These hits were predicted to have good ADMET properties. Finally, the in vivo study of cytotoxicity undertaken on Artemia salina larvae showed, in particular, through the evaluation of the LC50 / IC50 ratio that the six hits have a greater inhibitory activity than their toxic effect, which can thus be used as starting structures for the optimization and design of new AD drug candidates.
Note de contenu :
Annexes.Diplôme : Doctorat en sciences En ligne : ../theses/biologie/MOK7666.pdf Format de la ressource électronique : Permalink : index.php?lvl=notice_display&id=11500 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité MOK/7666 MOK/7666 Thèse Bibliothèque principale Thèses Disponible
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 : 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) Catégories : Français - Anglais
ChimieTags : 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 الكينولونات تحلق آزا-ميكائيل السائل الأيوني كينازولينات كينازولينونات كينولين بيرانوبيرازول بيريميدين تاكرين مرض
الألزهايمرIndex. 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 : index.php?lvl=notice_display&id=10221 Synthèse et caractérisation de poly-hétérocycles bioactifs [texte imprimé] / Chamseddine Derabli, Auteur ; Raouf Boulcina, Directeur de thèse . - جامعة الإخوة منتوري قسنطينة, 2016 . - 217 f. ; 30 cm.
2 copies imprimées disponibles
Langues : Français (fre)
Catégories : Français - Anglais
ChimieTags : 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 الكينولونات تحلق آزا-ميكائيل السائل الأيوني كينازولينات كينازولينونات كينولين بيرانوبيرازول بيريميدين تاكرين مرض
الألزهايمرIndex. 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 : index.php?lvl=notice_display&id=10221 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité DER/6892 DER/6892 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
