1372546-35-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors
Axford, Lorraine C.,Agarwal, Piyush K.,Anderson, Kelly H.,Andrau, Laura N.,Atherall, John,Barker, Stephanie,Bennett, James M.,Blair, Michael,Collins, Ian,Czaplewski, Lloyd G.,Davies, David T.,Gannon, Carlie T.,Kumar, Dushyant,Lancett, Paul,Logan, Alastair,Lunniss, Christopher J.,Mitchell, Dale R.,Offermann, Daniel A.,Palmer, James T.,Palmer, Nicholas,Pitt, Gary R.W.,Pommier, Stéphanie,Price, Daniel,Narasinga Rao,Saxena, Rashmi,Shukla, Tarun,Singh, Amit K.,Singh, Mahipal,Srivastava, Anil,Steele, Christopher,Stokes, Neil R.,Thomaides-Brears, Helena B.,Tyndall, Edward M.,Watson, David,Haydon, David J.
, p. 6598 - 6603 (2014/01/06)
The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Haemophilus influenzae. Further refinements to the scaffold designed to enhance drug-likeness included analogues bearing an α-substituent to the carboxylic acid group, resulting in excellent solubility and favourable pharmacokinetic properties.
ANTIBACTERIAL COMPOUNDS
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Page/Page column 44; 48, (2012/04/18)
The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
