کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1393518 1501220 2007 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14α-demethylase (CYP51)
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14α-demethylase (CYP51)
چکیده انگلیسی

A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substitutedphenyl)-piperazin-1-yl]-propan-2-ols have been designed and synthesized on the basis of the structure–activity relationships and antimycotic mechanism of azole antifungal agents. Their structures were confirmed by elemental analysis, IR, MS and 1H NMR. Results of preliminary antifungal tests against eight human pathogenic fungi (Candida albicans, Candida parapsilosis, Candida tropicalis, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton rubrum, Fonsecaea compacta, and Microsporum gypseum) in vitro showed that all title compounds exhibited activity against fungi tested to some extent. Among the compounds tested, all compounds showed higher activity against C. albicans than fluconazole in vitro. Compounds 3, 6–8, 28, 29, and 32 exhibited the same activities against C. albicans as voriconazole (with the MIC value of 0.0152 μg/mL). Compounds 3, 6, and 7 showed higher activity against C. parapsilosis than all five positive controls.

A series of novel triazole derivatives have been designed and synthesized. Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that all title compounds exhibited activity against fungi tested to some extent.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 42, Issue 9, September 2007, Pages 1226–1233
نویسندگان
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