Biaryl Ether Retrohydroxamates as Potent, Long-lived, Orally Bioavailable MMP Inhibitors

Michael R. Michaelides,Joseph F. Dellaria,Jane Gong,James H. Holms,Jennifer J. Bouska,Jamie Stacey,Carol K. Wada,H.Robin Heyman,Michael L. Curtin,Yan Guo,Carole L. Goodfellow,Ildiko B. Elmore,Daniel H. Albert,Terrance J. Magoc,Patrick A. Marcotte,Douglas W. Morgan,Steven K. Davidsen

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

A novel series of biaryl ether reverse hydroxamate MMP inhibitors has been developed. These compounds are potent MMP-2 inhibitors with limited activity against MMP-1. Select members of this series exhibit excellent pharmacokinetic properties with long elimination half-lives (7 h) and high oral bioavailability (100%).

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关键词

bioavailable mmp inhibitors,ether,long-lived

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