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J Med Chem. 2004 Jun 3;47(12):2981-3.

Sultam hydroxamates as novel matrix metalloproteinase inhibitors.

Author information

1
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. robert.cherney@bms.com

Abstract

In this communication we describe the design, synthesis, and evaluation of novel sultam hydroxamates 4 as MMP-2, -9, and -13 inhibitors. Compound 26 was found to be an active inhibitor (MMP-2 IC(50) = 1 nM) with 1000-fold selectivity over MMP-1 and good oral bioavailability (F = 43%) in mouse. An X-ray crystal structure of 26 in MMP-13 confirms the key hydrogen bonds and prime side binding in the active site.

PMID:
15163180
DOI:
10.1021/jm049833g
[Indexed for MEDLINE]

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