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Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation.

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.

SUBMITTER: Jachak GR

PROVIDER: S-EPMC4645241 | biostudies-literature | 2015 Nov

REPOSITORIES: biostudies-literature

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Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation.

Jachak Gorakhnath R GR Ramesh Remya R Sant Duhita G DG Jorwekar Shweta U SU Jadhav Manjusha R MR Tupe Santosh G SG Deshpande Mukund V MV Reddy D Srinivasa DS

ACS medicinal chemistry letters 20150922 11

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 fenpro ...[more]

PMID: 26617963

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