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The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.

作者信息

Steinman D H, Curtin M L, Garland R B, Davidsen S K, Heyman H R, Holms J H, Albert D H, Magoc T J, Nagy I B, Marcotte P A, Li J, Morgan D W, Hutchins C, Summers J B

机构信息

Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA.

出版信息

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2087-92. doi: 10.1016/s0960-894x(98)00396-5.

DOI:10.1016/s0960-894x(98)00396-5
PMID:9873491
Abstract

A series of succinate-derived hydroxamic acids incorporating a macrocyclic ring were designed, synthesized, and evaluated as inhibitors of matrix metalloproteinases. The inhibitors were designed based on the published X-ray crystal structure of batimastat (1) complexed with human neutrophil collagenase (MMP-8). The synthesized compounds were shown to inhibit selected MMPs in vitro with low nanomolar potency.

摘要

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