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High-throughput-screening-based identification and structure-activity relationship characterization defined (S)-2-(1-aminoisobutyl)-1-(3-chlorobenzyl) benzimidazole as a highly antimycotic agent nontoxic to cell lines

: Bauer, J.; Kinast, S.; Burger-Kentischer, A.; Finkelmeier, D.; Kleymann, G.; Rayyan, W.A.; Schröppel, K.; Singh, A.; Jung, G.; Wiesmüller, K.-H.; Rupp, S.; Eickhoff, H.


Journal of medicinal chemistry 54 (2011), No.19, pp.6993-6997
ISSN: 0022-2623
ISSN: 1520-4804
Journal Article
Fraunhofer IGB ()

Novel nontoxic (S)-2-aminoalkylbenzimidazole derivatives were found to be effective against Candida spp. at low micromolar concentrations using high-throughput screening with infected HeLa cells. A collection of analogues defined the chemical groups relevant for activity. The most active compound was characterized by transcriptional analysis of the response of C. albicans Sc5314. (S)-2-(1-Aminoisobutyl)-1-(3-chlorobenzyl)benzimidazole had a strong impact on membrane biosynthesis. Testing different clinically relevant pathogenic fungi showed the selectivity of the antimycotic activity against Candida species.