Design and Synthesis of 14α-Methyl-15-aza-D-homosterols as Novel Antimycotics

Roland E. Dolle, Lawrence I. Kruse, H. S. Allaudeen

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

A novel series of 14α-methyl-15-aza-D-homosterols 3-7 has been synthesized. These compounds display significant antimycotic activity in vitro (MIC = 0.8-3.1 µg/mL) that compares quite favorably to the activity observed for fluconazole (MIC = 0.8 µg/mL). Azasterols 3 and 4 were active in vivo as reflected in the increased survival time of Candida albicans infected mice. The antimycotic activity of 3-7 is hypothesized to be a consequence of the inhibition of fungal 14,15-sterol reductase.

Original languageEnglish
Pages (from-to)877-880
Number of pages4
JournalJournal of Medicinal Chemistry
Volume33
Issue number2
DOIs
StatePublished - Feb 1990

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