371228-10-3Relevant articles and documents
Discovery of novel bacterial elongation condensing enzyme inhibitors by virtual screening
Zheng, Zhong,Parsons, Joshua B.,Tangallapally, Rajendra,Zhang, Weixing,Rock, Charles O.,Lee, Richard E.
, p. 2585 - 2588 (2014)
The elongation condensing enzymes in the bacterial fatty acid biosynthesis pathway represent desirable targets for the design of novel, broad-spectrum antimicrobial agents. A series of substituted benzoxazolinones was identified in this study as a novel class of elongation condensing enzyme (FabB and FabF) inhibitors using a two-step virtual screening approach. Structure activity relationships were developed around the benzoxazolinone scaffold showing that N-substituted benzoxazolinones were most active. The benzoxazolinone scaffold has high chemical tractability making this chemotype suitable for further development of bacterial fatty acid synthesis inhibitors.