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• W2950651198 abstract "Prior reports from our laboratories have identified the nonpeptidic inhibitor 2 as a potent and selective Cathepsin K (Cat K) inhibitor. Modelling studies suggested that the introduction of a NH linker between the P3 aryl and P2 leucinamide moieties would allow the formation of a H-bond with the Gly66 residue of Cat K, hopefully increasing potency. Aniline 4 was thus synthesized and showed improved potency over its predecessor 2. Further modelling concluded that a 2-substituted five membered ring could more adequately place the P3 moiety of 4 into the S3 pocket of Cat K. The synthesis of the 2-substituted thiophene 5 confirmed this hypothesis by displaying a slight increase in potency against Cat K (>10-fold increase in potency vs 2) and a good selectivity profile against Cathepsins B, L, and S. This rationally designed inhibitor 5 also displayed increased potency in a functional bone resorption assay (10 nM) versus 2 (95 nM)." @default.
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• W2950651198 date "2004-08-01" @default.
• W2950651198 modified "2023-09-27" @default.
• W2950651198 title "Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors" @default.
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• W2950651198 doi "https://doi.org/10.1016/j.bmcl.2004.05.087" @default.
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