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Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
TLDR
Pharmacokinetic evaluation of 12 members of this series of potent and selective inhibitors of cysteine protease cathepsin K indicated that some members could be suitable candidates to develop new orally active therapeutic agents for the treatment of osteoporosis.
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 was