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Bioorg Med Chem Lett. 2001 Aug 20;11(16):2147-51.

N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.

Author information

1
GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA. dm12907@glaxowellcome.com

Abstract

N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and TNF-alpha converting enzyme (TACE). Compound 13c possesses good oral and intravenous pharmacokinetics in the rat and dog.

PMID:
11514157
DOI:
10.1016/s0960-894x(01)00377-8
[Indexed for MEDLINE]

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