Volume 32, Issue 45
Natural Products
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ChemInform Abstract: N-Hydroxyformamide Peptidomimetics as TACE/Matrix Metalloprotease Inhibitors: Oral Activity via P1′ Isobutyl Substitution.

David L. Musso

David L. Musso

GlaxoSmithKline Res. Dev., Research Triangle Park, NC 27709, USA

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et al. et al.

et al. et al.

GlaxoSmithKline Res. Dev., Research Triangle Park, NC 27709, USA

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First published: 23 May 2010

Abstract

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ChemInform Abstract

Eleven tripeptidomimetics like (I) are synthesized and their potential as TNF-α converting enzyme (TACE) and matrix metalloprotease inhibitors in vitro and in vivo is examined. Peptidomimetic (Ia) is further evaluated for its pharmacokinetic properties. Upon intravenous and oral dosing, (Ia) exhibits good half-life and bioavailability.

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