Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.

Abstract:

:Cathepsin K is highly expressed in human osteoclasts, and is implicated in bone resorption. This makes it an attractive target for the treatment of osteoporosis. Peptides containing 2-amino-1'-hydroxymethyl ketones and 2-amino-1'-alkoxymethyl ketones were discovered as potent inhibitors of cathepsin K. A novel synthetic route was devised to facilitate rapid elucidation of the SAR of these inhibitors. The synthesis and SAR of hydroxymethyl ketones are presented.

journal_name

Bioorg Med Chem Lett

authors

Mendonca RV,Venkatraman S,Palmer JT

doi

10.1016/s0960-894x(02)00611-x

subject

Has Abstract

pub_date

2002-10-21 00:00:00

pages

2887-91

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960894X0200611X

journal_volume

12

pub_type

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