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Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3.

作者信息

Reiter Lawrence A, Mitchell Peter G, Martinelli Gary J, Lopresti-Morrow Lori L, Yocum Sue A, Eskra James D

机构信息

Pfizer Inc, Global Reseach & Development, Groton Laboratories, Eastern Point Rd., 06340, Groton, CT, USA.

出版信息

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2331-6. doi: 10.1016/s0960-894x(03)00413-x.

DOI:10.1016/s0960-894x(03)00413-x
PMID:12824028
Abstract

Phosphinic acid-based inhibitors of MMP-13 have been investigated with the aim of identifying potent inhibitors with high selectivity versus MMP-1. Independent variation of the substituents on a P(1)' phenethyl group and a P(2) benzyl group improved potencies in both cases around 3-fold over the unsubstituted parent. Combining improved P(1)' and P(2) groups into a single molecule gave an inhibitor with a 4.5 nM IC(50) against MMP-13 and which is 270-fold selective over MMP-1.

摘要

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