Antifungal activity of synthetic di(hetero)arylamines based on the benzo[b]thiophene moiety
Antifungal activity of synthetic di(hetero)arylamines based on the benzo[b]thiophene moiety
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DOI：
10.1016/j.bmc.2008.07.042
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发表时间：
2008-09-01
影响因子：
3.5
通讯作者：
Kirsch, Gilbert
中科院分区：
文献类型：
--
作者：
Pinto, Eugenia;Queiroz, Maria-Joao R. P.;Kirsch, Gilbert
通过基于CLSI（前身为NCCLS）指南的肉汤大量稀释试验，评价了苯并[B]噻吩系统的几种二（杂）芳胺衍生物对临床相关念珠菌属、曲霉属和皮肤真菌种属的抗真菌活性。活性最高的化合物显示出广谱活性（针对所有测试的真菌菌株，包括氟康唑耐药真菌），对皮肤癣菌的MIC特别低。抑制白念珠菌二态转化和流式细胞术研究的结果进一步证实了它们的生物活性。通过这项研究，有可能建立一些结构-活性关系（SAR）。羟基基团被证明是必不可少的活性的芳基衍生物。此外，在吡啶衍生物的活性谱拓宽了苯并[B]噻吩系统的位置2上的酯基的情况下。(C)2008爱思唯尔有限公司保留所有权利。
The antifungal activity of several di(hetero)arylamine derivatives of the benzo[b]thiophene system was evaluated against clinically relevant Candida, Aspergillus, and dermatophyte species by a broth macrodilution test based on CLSI ( formerly NCCLS) guidelines. The most active compound showed a broad spectrum of activity ( against all tested fungal strains, including fluconazole-resistant fungi), with particularly low MICs for dermatophytes. Results from the inhibition of the dimorphic transition in Candida albicans and flow cytometry studies further confirmed their biological activity. With this study it was possible to establish some structure-activity relationships (SARs). The hydroxy groups proved to be essential for the activity in the aryl derivatives. Furthermore, the spectrum of activity in the pyridine derivatives was broadened by the absence of the ester group on position 2 of the benzo[b]thiophene system. (C) 2008 Elsevier Ltd. All rights reserved.