1459772-53-2Relevant academic research and scientific papers
Monocycle gyrase and topoisomerase IV inhibitor
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Paragraph 0346; 0347-0349, (2017/01/05)
The invention belongs to the technical field of medicines, and in particular relates to a gyrase and topoisomerase IV inhibitor compound of formula (I) as shown in the specification, and a pharmaceutically acceptable salt, an ester or stereoisomers thereo
Discovery and in vivo evaluation of alcohol-containing benzothiazoles as potent dual-targeting bacterial DNA supercoiling inhibitors
Palmer, James T.,Axford, Lorraine C.,Barker, Stephanie,Bennett, James M.,Blair, Michael,Collins, Ian,Davies, David T.,Ford, Leigh,Gannon, Carlie T.,Lancett, Paul,Logan, Alastair,Lunniss, Christopher J.,Morton, Craig J.,Offermann, Daniel A.,Pitt, Gary R.W.,Rao, B. Narasinga,Singh, Amit K.,Shukla, Tarun,Srivastava, Anil,Stokes, Neil R.,Thomaides-Brears, Helena B.,Yadav, Anju,Haydon, David J.
, p. 4215 - 4222 (2014/10/15)
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.
Antibacterial Compounds
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Paragraph 0536, (2013/10/07)
The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
