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DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: Synthesis and antibacterial activity |
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| Authors: | Stephen P East Clara Bantry White Oliver Barker Stephanie Barker James Bennett David Brown E Andrew Boyd Christopher Brennan Chandana Chowdhury Ian Collins Emmanuelle Convers-Reignier Brian W Dymock Rowena Fletcher David J Haydon Mihaly Gardiner Stuart Hatcher Peter Ingram Paul Lancett Paul Mortenson Konstantinos Papadopoulos Lloyd G Czaplewski |
| Institution: | 1. Evotec (UK) Ltd, Discovery Services, 114 Milton Park, Abingdon, Oxfordshire OX14 4SA, UK;2. Prolysis Ltd, Oxford University Begbroke Science Park, Sandy Lane, Yarnton, Oxfordshire OX5 1PF, UK |
| Abstract: | The synthesis and antibacterial activities of three chemotypes of DNA supercoiling inhibitors based on imidazolo1,2-a]pyridine and 1,2,4]triazolo1,5-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. |
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