Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10590975 | Bioorganic & Medicinal Chemistry Letters | 2014 | 8 Pages |
Abstract
A series of dual-targeting, alcohol-containing benzothiazoles has been identified with superior antibacterial activity and drug-like properties. Early lead benzothiazoles containing carboxylic acid moieties showed efficacy in a well-established in vivo model, but inferior drug-like properties demanded modifications of functionality capable of demonstrating superior efficacy. Eliminating the acid group in favor of hydrophilic alcohol moieties at C5, as well as incorporating solubilizing groups at the C7 position of the core ring provided potent, broad-spectrum Gram-positive antibacterial activity, lower protein binding, and markedly improved efficacy in vivo.
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Authors
James T. Palmer, Lorraine C. Axford, Stephanie Barker, James M. Bennett, Michael Blair, Ian Collins, David T. Davies, Leigh Ford, Carlie T. Gannon, Paul Lancett, Alastair Logan, Christopher J. Lunniss, Craig J. Morton, Daniel A. Offermann,