Bioorganic and Medicinal Chemistry Letters p. 2087 - 2092 (1998)
Update date:2022-08-04
Topics:
Steinman, Douglas H.
Curtin, Michael L.
Garland, Robert B.
Davidsen, Steven K.
Heyman, H. Robin
Holms, James H.
Albert, Daniel H.
Magoc, Terry J.
Nagy, Ildiko B.
Marcotte, Patrick A.
Li, Junling
Morgan, Douglas W.
Hutchins, Charles
Summers, James B.
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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