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Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
The synthesis and biological profile of a novel series of potent and selective inhibitors of cysteine protease cathepsin K (Cat K) are described. Pharmacokinetic evaluation of 12 indicated that someExpand
Identification of metabolites of the tryptase inhibitor CRA-9249: observation of a metabolite derived from an unexpected hydroxylation pathway.
The metabolites of the tryptase inhibitor CRA-9249 were identified after exposure to liver microsomes. CRA-9249 was found to be degraded rapidly in liver microsomes from rabbit, dog, cynomolgusExpand
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P3 elements for potency and selectivity.
The synthesis of a series of highly potent and selective inhibitors of cathepsin K based on the 3,4-disubstituted azetidin-2-one warhead is reported. A high degree of potency and selectivity wasExpand
Does Delivery Length Impact Measures of Whole-Body Biomechanical Load During Pace Bowling?
PURPOSE To investigate whether changes in delivery length (ie, short, good, and full) lead to alterations in whole-body biomechanical loading as determined by ground reaction force during front-footExpand