| Structure - Activity Relationships of 2-Benzylsulfanylbenzothiazoles: Synthesis and Selective Antimycobacterial Properties. | |
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MedLine Citation:
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PMID: 22385183 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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A set of 2-benzylsulfanyl derivatives of benzothiazole was synthesized and evaluated for antimicrobial andm cytotoxic activities. The biological screening on antimicrobial activity against a panel of Gram-positive and Gramnegative bacteria, yeasts and fungi identified benzylsulfanyl derivatives of benzothiazole as selective inhibitors of mycobacteria. The lead compounds in the set, dinitro derivatives exhibited significant activity against sensitive and multidrug-resistant strains of M. tuberculosis and low cytotoxicity. The QSAR study indicated that the antituberculotic activity is connected with LUMO and HOMO energies. The lower lipophilicity and the increased size of the molecule contribute to nantituberculotic activity. Thus, dinitrobenzylsulfanyl derivatives of benzothiazole represent promising smallmolecule synthetic antimycobacterials. |
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Authors:
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Vera Klimesová; Jan Kocí; Karel Palát; Jirina Stolaríková; Hans-Martin Dahse; Ute Möllmann |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-2-24 |
Journal Detail:
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Title: Medicinal chemistry (Shariqah (United Arab Emirates)) Volume: - ISSN: 1875-6638 ISO Abbreviation: - Publication Date: 2012 Feb |
Date Detail:
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Created Date: 2012-3-5 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101240303 Medline TA: Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, Hradec Králové, 500 05, Czech Republic. vera.klimesova@faf.cuni.cz. |
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