Jachak, Gorakhnath R. ; Ramesh, Remya ; Sant, Duhita G. ; Jorwekar, Shweta U. ; Jadhav, Manjusha R. ; Tupe, Santosh G. ; Deshpande, Mukund V. ; Reddy, D. Srinivasa (2015) Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation ACS Medicinal Chemistry Letters, 6 (11). pp. 1111-1116. ISSN 1948-5875
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Official URL: http://doi.org/10.1021/acsmedchemlett.5b00245
Related URL: http://dx.doi.org/10.1021/acsmedchemlett.5b00245
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. Sila-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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to American Chemical Society |
| ID Code: | 121944 |
| Deposited On: | 23 Jul 2021 09:25 |
| Last Modified: | 23 Jul 2021 09:25 |
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