DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: synthesis and antibacterial activity

…, C Chowdhury, I Collins, E Convers-Reignier…

Index: East, Stephen P.; White, Clara Bantry; Barker, Oliver; Barker, Stephanie; Bennett, James; Brown, David; Boyd, E. Andrew; Brennan, Christopher; Chowdhury, Chandana; Collins, Ian; Convers-Reignier, Emmanuelle; Dymock, Brian W.; Fletcher, Rowena; Haydon, David J.; Gardiner, Mihaly; Hatcher, Stuart; Ingram, Peter; Lancett, Paul; Mortenson, Paul; Papadopoulos, Konstantinos; Smee, Carol; Thomaides-Brears, Helena B.; Tye, Heather; Workman, James; Czaplewski, Lloyd G. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 894 - 899

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Citation Number: 45

Abstract

The synthesis and antibacterial activities of three chemotypes of DNA supercoiling inhibitors based on imidazolo [1, 2-a] pyridine and [1, 2, 4] triazolo [1, 5-a] pyridine scaffolds that target the ATPase subunits of DNA gyrase and topoisomerase IV (GyrB/ParE) is reported. The most potent scaffold was selected for optimization leading to a series with potent Gram- positive antibacterial activity and a low resistance frequency.