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Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design.
The design, synthesis, mPGES-1 activity and in vivo PK of a novel set of substituted benzoxazoles are described and a conformation-based hypothesis for mPGE(2) synthase1 activity based on the preferred conformation of the cyclohexane ring within this class of inhibitors is described. Expand
Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.
The first reported non-peptide small molecule inhibitors of both HGFA and hepsin are discovered, which have differential potency and selectivity towards all three proteases. Expand