期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 123, 期 -, 页码 514-522出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.07.067
关键词
Antifungal activity; Azole antifungals; CYP51; Structure-activity relationship
资金
- Program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in University
A series of compounds with benzothiazole and amide-imidazole scaffolds were designed and synthesized to combat the increasing incidence of drug-resistant fungal infections. The antifungal activity of these compounds was evaluated in vitro, and their structure-activity relationships (SARs) were evaluated. The synthesized compounds showed excellent inhibitory activity against Candida albicans and Cryptococcus neoformans. The most potent compounds 14o, 14p, and 14r exhibited potent activity, with minimum inhibitory concentration (MIC) values in the range of 0.125-2 mu g/mL. Preliminary mechanism studies revealed that the compound 14p might act by inhibiting the CYP51 of Candida albicans. The SARs and binding mode established in this study are useful for further lead optimization. (C) 2016 Elsevier Masson SAS. All rights reserved.
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