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

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

D H Steinman  1 , M L Curtin, R B Garland, S K Davidsen, H R Heyman, J H Holms, D H Albert, T J Magoc, I B Nagy, P A Marcotte, J Li, D W Morgan, C Hutchins, J B Summers
Affiliations

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

D H Steinman et al. Bioorg Med Chem Lett. .

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.

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