459190-08-0Relevant articles and documents
Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors
Geng, Bolin,Comita-Prevoir, Janelle,Eyermann, Charles J.,Reck, Folkert,Fisher, Stewart
, p. 5432 - 5435 (2011/10/12)
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.