Novel antifungals based on 4-substituted imidazole: A combinatorial chemistry approach to lead discovery and optimization

Bioorganic & Medicinal Chemistry Letters
2000.0

Abstract

A series of 4-substituted imidazole sulfonamides has been prepared by solid-phase chemistry. These compounds were found to have good in vitro antifungal activity and constitute the first examples of C-linked azoles with such activity. The most potent inhibitor (30) demonstrated inhibition of key Candida strains at an in vitro concentration of < 100nM and compared favorably with in vitro potency of itraconazole.

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