1428147-73-2Relevant articles and documents
Antagonism of a zinc metalloprotease using a unique metal-chelating scaffold: Tropolones as inhibitors of P. aeruginosa elastase
Fullagar, Jessica L.,Garner, Amanda L.,Struss, Anjali K.,Day, Joshua A.,Martin, David P.,Yu, Jing,Cai, Xiaoqing,Janda, Kim D.,Cohen, Seth M.
supporting information, p. 3197 - 3199 (2013/05/08)
Tropolone emerged from the screening of a chelator fragment library (CFL) as an inhibitor of the Zn2+-dependent virulence factor, Pseudomonas aeruginosa elastase (LasB). Based on this initial hit, a series of substituted tropolone-based LasB inhibitors was prepared, and a compound displaying potent activity in vitro and in a bacterial swarming assay was identified. Importantly, this inhibitor was found to be specific for LasB over other metalloenzymes, validating the usage of tropolone as a viable scaffold for identifying first-in-class LasB inhibitors.