Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors

…, JM Bennett, M Blair, I Collins, LG Czaplewski…

文献索引：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, Stephanie; 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. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6598 - 6603

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被引用次数: 11

摘要

Abstract 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- ...