ChemInform Abstract: N-Hydroxyformamide Peptidomimetics as TACE/Matrix Metalloprotease Inhibitors: Oral Activity via P1′ Isobutyl Substitution.
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.