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Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).

Abstract：

: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 (1)H 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 0.0152microg/mL). Compounds 3, 6, and 7 showed higher activity against C. parapsilosis than all five positive controls.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Sun QY,Xu JM,Cao YB,Zhang WN,Wu QY,Zhang DZ,Zhang J,Zhao HQ,Jiang YY

doi

10.1016/j.ejmech.2007.01.006

subject

Has Abstract

pub_date

2007-09-01 00:00:00

pages

1226-33

issue

9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00043-8

journal_volume

42

pub_type

杂志文章

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