| 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. | |
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MedLine Citation:
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PMID: 21711055 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: JOURNAL ARTICLE Date: 2011-6-29 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: - ISSN: 1520-4804 ISO Abbreviation: - Publication Date: 2011 Jun |
Date Detail:
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Created Date: 2011-6-29 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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