Discovery and optimization of Benzenesulfonanilide (cas 1678-25-7) derivatives as a novel class of 11β-HSD1 inhibitors
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Add time:09/24/2019 Source:sciencedirect.com
A novel series of Benzenesulfonanilide (cas 1678-25-7) 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).
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