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Bioorg Med Chem Lett. 2003 Jun 16;13(12):2051-3.

3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.

Author information

1
Department of Medicinal Chemisty, Celera, 180 Kimball Way, South San Francisco, CA 94080, USA. setti@celera.com

Abstract

A novel series of 3,4-disubstituted azetidinones based inhibitors of the cysteine protease cathepsin K (Cat K) has been identified. Although not optimized, some of these compounds show at least 100-fold selectivity against other cathepsins. The use of cyclic moieties as P2 elements has proven to be crucial to achieve a high degree of selectivity.

PMID:
12781193
DOI:
10.1016/s0960-894x(03)00304-4
[Indexed for MEDLINE]

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