| Inhibition of the β-class carbonic anhydrases from Mycobacterium tuberculosis with carboxylic acids. | |
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MedLine Citation:
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PMID: 22299588 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The growth of Mycobacterium tuberculosis is strongly inhibited by weak acids although the mechanism by which these compounds act is not completely understood. A series of substituted benzoic acids, nipecotic acid, ortho- and para-coumaric acid, caffeic acid and ferulic acid were investigated as inhibitors of three β-class carbonic anhydrases (CAs, EC 4.2.1.1) from this pathogen, mtCA 1 (Rv1284), mtCA 2 (Rv3588c) and mtCA 3 (Rv3273). All three enzymes were inhibited with efficacies between the submicromolar to the micromolar one, depending on the scaffold present in the carboxylic acid. mtCA 3 was the isoform mostly inhibited by these compounds (K(I)s in the range of 0.11-0.97 µM); followed by mtCA 2 (K(I)s in the range of 0.59-8.10 µM), whereas against mtCA 1, these carboxylic acids showed inhibition constants in the range of 2.25-7.13 µM. This class of relatively underexplored β-CA inhibitors warrant further in vivo studies, as they may have the potential for developing antimycobacterial agents with a diverse mechanism of action compared to the clinically used drugs for which many strains exhibit multi-drug or extensive multi-drug resistance. |
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Authors:
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Alfonso Maresca; Daniela Vullo; Andrea Scozzafava; Gheorghe Manole; Claudiu T Supuran |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-2-3 |
Journal Detail:
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Title: Journal of enzyme inhibition and medicinal chemistry Volume: - ISSN: 1475-6374 ISO Abbreviation: - Publication Date: 2012 Feb |
Date Detail:
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Created Date: 2012-2-3 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101150203 Medline TA: J Enzyme Inhib Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica , Sesto Fiorentino (Florence) , Italy. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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