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

Autor: 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.
Přispěvatelé: Publica
Jazyk: angličtina
Rok vydání: 2011
Popis: 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.
Databáze: OpenAIRE