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

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