1区 · 医学
Article
作者: Bauer, Joerg ; Kinast, Stephan ; Burger-Kentischer, Anke ; Finkelmeier, Doris ; Kleymann, Gerald ; Abu Rayyan, Walid ; Schroppel, Klaus ; Singh, Anurag ; Jung, Guenther ; Wiesmuller, Karl-Heinz ; Rupp, Steffen ; Eickhoff, Holger
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.