Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors

B Geng, J Comita-Prevoir, CJ Eyermann, F Reck…

Index: Geng, Bolin; Comita-Prevoir, Janelle; Eyermann, Charles J.; Reck, Folkert; Fisher, Stewart Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5432 - 5435

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Citation Number: 21

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.