期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 6, 期 11, 页码 1111-1116出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00245
关键词
Antifungal drugs; Candida albicans; ergosterol biosynthesis; morpholines; sila-analogues
资金
- CSIR-NCL, Pune - Department of Biotechnology, India [BT/PR7442/MED/29/680/2012]
- CSIR, New Delhi under XII Five Year Plan SMILE program [CSC0111]
- CSIR, India
Known morpholine class antifungals (fenpropimorph, fenpropidin, and amorolfine) were synthetically modified through silicon incorporation to have 15 sila-analogues. Twelve sila-analogues exhibited potent antifungal activity against different human fungal pathogens such as Candida albicans, Candida glabrata, Candida tropicalis, Cryptococcus neoformans, and Aspergillus niger. Si la-analogue 24 (fenpropimorph analogue) was the best in our hands, which showed superior fungicidal potential than fenpropidin, fenpropimorph, and amorolfine. The mode of action of sila-analogues was similar to morpholines, i.e., inhibition of sterol reductase and sterol isomerase enzymes of ergosterol synthesis pathway.
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