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  4. 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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2011
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Titel

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

Abstract
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.
Author(s)
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.
Zeitschrift
Journal of medicinal chemistry
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DOI
10.1021/jm200571e
Language
Englisch
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