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العنوان
Synthesis of some novel 1,2,4 triazole and fused triazole derivatives as antimicrobial, antiviral and cytotoxic agents /
المؤلف
Abd El-Hay, Sherin Mohamed.
هيئة الاعداد
باحث / شيرين محمد عبدالحى
مشرف / حسن محمد عيسى
مشرف / محمد عادل مسعود
مشرف / ليلى أبوزيد
الموضوع
Triazoles.
تاريخ النشر
2009.
عدد الصفحات
202 p. :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
العلوم الصيدلية
تاريخ الإجازة
01/01/2009
مكان الإجازة
جامعة المنصورة - كلية الصيدلة - Department of pharmacology organic chemistry
الفهرس
Only 14 pages are availabe for public view

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Abstract

Literature revealed the promising role of 1,2,4-triazoles and their fused derivatives as potential antimicrobial, antiviral, and cytotoxic agents In the present investigation, new series of (E)-2-(3-((E)-substituted-benzylideneamino)-1H-1,2,4-triazol-5-ylthio)-N’-(4-fluorobenzylidene) acetohydrazide, (E)-5-((5-(alkyl/arylthio)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl)methylthio)-N-(4-fluorobenzylidene)-1H-1,2,4-triazol-3-amine, 2-((5-(alkyl/aryllthio)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-yl)methylthio)-5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine, 2-(5,7-Disubstituted-1,2,4]triazolo[1,5-a]pyrimidin-2-ylthio)-1-(-substituted-piperazin-1-yl)ethanones,2-(7-Chloro-6-(4-phenylpiperazine-1-carbonyl)-1,2,4-triazolo[1,5-a]pyrimidin-2-ylthio)-1-(4-phenylpiperazin-1-yl) ethanones and 7-(2-Oxo-2-(4-phenylpiperazin-1-yl)ethylthio)-2-phenyl-2-substituted-2H-pyrazolo[4,3-e] 1,2,4-triazolo[1,5-a]pyrimidin-3(5H)-one systems were prepared in order to obtain the target compounds, different chemical pathways were adopted. Thirty three novel compounds that are not mentioned in the available literature were synthesized. The formation and purity of the newly synthesized compounds were checked by TLC, and their structures were elucidated through elemental microanalyses, IR, 1H-NMR and mass spectroscopy. All the thirty three compounds were screened as antimicrobial. Twenty two compounds were screened as antitumor and antiviral. Compound (70a) showed the highest antiviral activity. Molecular modeling studies were used to assess the complementarity of the tested compounds within the binding pocket of the cytochrome P450 as inhibitors in comparison with the antifungal Fluconazole to evaluate their recognition profiles at the CYP51 binding-pocket.