Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity

A K Saha; L Liu; P Marichal; F Odds

doi:10.1016/s0960-894x(00)00551-5

Novel antifungals based on 4-substituted imidazole: solid-phase synthesis of substituted aryl sulfonamides towards optimization of in vitro activity

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2735-9. doi: 10.1016/s0960-894x(00)00551-5.

Authors

A K Saha¹, L Liu, P Marichal, F Odds

Affiliation

¹ Drug Discovery, Janssen Research Foundation, Spring House, PA 19477, USA.

PMID: 11133080
DOI: 10.1016/s0960-894x(00)00551-5

Abstract

The in vitro activity of novel 4-substituted imidazole antifungals was optimized by solid-phase chemistry and parallel synthesis. Potent yeast-selective as well as broad-spectrum antifungal compounds (32 and 20) were discovered.

MeSH terms

Antifungal Agents / chemical synthesis*
Antifungal Agents / pharmacology
Candida albicans / drug effects
Fungi / drug effects
Imidazoles / chemical synthesis
Imidazoles / pharmacology*
Microbial Sensitivity Tests
Structure-Activity Relationship
Sulfonamides / chemical synthesis
Sulfonamides / pharmacology
Yeasts / drug effects

Substances

Antifungal Agents
Imidazoles
Sulfonamides