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Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors
Authors:Geng Bolin  Comita-Prevoir Janelle  Eyermann Charles J  Reck Folkert  Fisher Stewart
Institution:Infection Innovative Medicines, AstraZeneca R&D Boston, Waltham, MA 02451, USA. bolin.geng@astrazeneca.com
Abstract:An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity.
Keywords:Antibacterials  4-Amino-piperidines  DNA gyrase  Topoisomerase IV  Type IIa topoisomerases
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