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Greater Noida, India

Palmer J.T.,Biota Scientific Management | Axford L.C.,Biota Scientific Management | Barker S.,Biota Europe Ltd | Bennett J.M.,Biota Europe Ltd | And 19 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

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 C 5, 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. © 2014 Elsevier Ltd. All rights reserved.

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