Silicon incorporated morpholine antifungals: design, synthesis, and biological evaluation
Title | Silicon incorporated morpholine antifungals: design, synthesis, and biological evaluation |
Publication Type | Journal Article |
Year of Publication | 2015 |
Authors | Jachak, GR, Ramesh, R, Sant, DG, Jorwekar, SU, Jadhav, MR, Tupe, SG, Deshpande, MV, D. Reddy, S |
Journal | ACS Medicinal Chemistry Letters |
Volume | 6 |
Issue | 11 |
Pagination | 1111-1116 |
Date Published | NOV |
ISSN | 1948-5875 |
Keywords | Antifungal drugs, Candida albicans, ergosterol biosynthesis, morpholines, sila-analogues |
Abstract | 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. |
DOI | 10.1021/acsmedchemlett.5b00245 |
Type of Journal (Indian or Foreign) | Foreign |
Impact Factor (IF) | 3.355 |