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 |
