1380539-64-9Relevant academic research and scientific papers
Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11β-HSD1 inhibitors
Rew, Yosup,Degraffenreid, Michael,He, Xiao,Jaen, Juan C.,McMinn, Dustin L.,Sun, Daqing,Tu, Hua,Ursu, Stefania,Powers, Jay P.
, p. 3786 - 3790 (2012/07/14)
A novel series of benzenesulfonanilide derivatives of 11β-HSD1 inhibitors were identified via modification of the sulfonamide core of the arylsulfonylpiperazine lead structures. The synthesis, in vitro biological evaluation, and structure-activity relationship of these compounds are presented. Optimization of this series rapidly resulted in the discovery of compounds (S)-10 and (S)-23 (11β-HSD1 SPA IC50 = 1.8 and 1.4 nM, respectively).
