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Novel antifungals based on 4-substituted imidazole: a combinatorial chemistry approach to lead discovery and
A K Saha1, L Liu, R L Simoneaux
1Drug Discovery, Janssen Research Foundation, Spring House, PA 19477, USA. asaha@prius.jnj.com
Bioorganic & Medicinal Chemistry Letters
|September 30, 2000
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.