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设计、合成及一些新的咪唑和三唑衍生物的抗真菌活性。

Design, synthesis and antifungal activity of some new imidazole and triazole derivatives.

机构信息

Department of Medicinal Chemistry, Shiraz University of Medical Sciences, Iran.

出版信息

Arch Pharm (Weinheim). 2011 Oct;344(10):658-65. doi: 10.1002/ardp.201000357. Epub 2011 Aug 25.

Abstract

Triazole and imidazole are incorporated into the structures of many antifungal compounds. In this study a novel series of 1,2,4-triazole, imidazole, benzoimidazole, and benzotriazole derivatives was designed as inhibitors of cytochrome P450 14α-demethylase (14DM). These structures were docked into the active site of MT-CYP51, using Autodock program. Sixteen compounds with the best binding energy were synthesized. The chemical structures of the new compounds were confirmed by elemental and spectral ((1) H-NMR and Mass) analyses. All compounds were investigated for antifungal activity against Candida albicans, Candida tropicalis, Candida glabrata, Candida parapeilosis, Candida kruzei, Candida dubliniensis, Aspergillus fomigatus, Aspergillus flavus, Microsporum canis, Microsporum gypseum, Trichophyton mentagrophyte, Epidermophyton floccosum. Some compounds showed excellent in-vitro antifungal activity against most of the tested fungi. Compounds 2, 9, and 10 had antifungal activity against several resistant fungi against fluconazole and itraconazole.

摘要

三唑和咪唑被整合到许多抗真菌化合物的结构中。在这项研究中,设计了一系列新型的 1,2,4-三唑、咪唑、苯并咪唑和苯并三唑衍生物作为细胞色素 P450 14α-脱甲基酶(14DM)的抑制剂。使用 Autodock 程序将这些结构对接进 MT-CYP51 的活性部位。合成了 16 种具有最佳结合能的化合物。通过元素分析和光谱(1H-NMR 和 Mass)分析确认了新化合物的化学结构。所有化合物均进行了抗真菌活性测试,以评估它们对白色念珠菌、热带念珠菌、光滑念珠菌、近平滑念珠菌、克鲁兹念珠菌、都柏林念珠菌、烟曲霉、黄曲霉、犬小孢子菌、石膏小孢子菌、须毛癣菌、絮状表皮癣菌的抑制作用。一些化合物对大多数测试真菌表现出优异的体外抗真菌活性。化合物 2、9 和 10 对几种对氟康唑和伊曲康唑耐药的真菌具有抗真菌活性。

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