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…

Index: 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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Citation Number: 11

Abstract

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- ...