Document Detail


High-throughput screening-based identification and structure-activity relationship-characterization defined (S)-2-(1-aminoisobutyl)-1-(3-chlorobenzyl) benzimidazole as a highly antimycotic agent, non-toxic to cell lines.
MedLine Citation:
PMID:  21711055     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Novel non-toxic (S)-2-aminoalkyl benzimidazole derivatives were found to be effective against Candida spp. at low micromolar concentrations using HTS 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.
Authors:
Jörg Bauer; Stephan Kinast; Anke Burger-Kentischer; Doris Finkelmeier; Gerald Kleymann; Walid Abu Rayyan; Klaus Schröppel; Anuragh Singh; Günther Jung; Karl-Heinz Wiesmüller; Steffen Rupp; Holger Eickhoff
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-29
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-6-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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