Antimicrobial Agents and Chemotherapy 1998-10-01

Structure-in vitro activity relationships of pentamidine analogues and dication-substituted bis-benzimidazoles as new antifungal agents.

M Del Poeta, W A Schell, C C Dykstra, S Jones, R R Tidwell, A Czarny, M Bajic, A Kumar, D Boykin, J R Perfect

Index: Antimicrob. Agents Chemother. 42(10) , 2495-502, (1998)

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Abstract

Twenty analogues of pentamidine, 7 primary metabolites of pentamidine, and 30 dicationic substituted bis-benzimidazoles were screened for their inhibitory and fungicidal activities against Candida albicans and Cryptococcus neoformans. A majority of the compounds had MICs at which 80% of the strains were inhibited (MIC80s) comparable to those of amphotericin B and fluconazole. Unlike fluconazole, many of these compounds were found to have potent fungicidal activity. The most potent compound against C. albicans had an MIC80 of