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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

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journal contribution
posted on 13.10.2011, 00:00 by Jörg Bauer, Stephan Kinast, Anke Burger-Kentischer, Doris Finkelmeier, Gerald Kleymann, Walid Abu Rayyan, Klaus Schröppel, Anurag Singh, Günther Jung, Karl-Heinz Wiesmüller, Steffen Rupp, Holger Eickhoff
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.