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Journal article

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.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acsmedchemlett.5b00245

Authors


More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Biology
Role:
Author


Publisher:
American Chemical Society
Journal:
ACS Medicinal Chemistry Letters More from this journal
Volume:
6
Issue:
11
Pages:
1111-1116
Publication date:
2015-09-22
Acceptance date:
2015-09-22
DOI:
ISSN:
1948-5875


Language:
English
Keywords:
Pubs id:
1278491
Local pid:
pubs:1278491
Deposit date:
2022-09-12

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