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Bioorg Med Chem Lett. 2005 Aug 15;15(16):3787-90.

Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors.

Author information

1
Department of Chemistry, Pfizer Global Research and Development, Fresnes Laboratories, 3-9 rue de la Loge, BP 100, F-94265 Fresnes Cedex, France. anne-claude.dublanchet@wanadoo.fr

Abstract

A new class of MMP-12 inhibitors was discovered and optimized using structure-based drug design methods. Modeling studies using a known MMP-12 crystal structure identified a new interaction mode for these new MMP-12 inhibitors. Further optimization resulted in the discovery of a compound displaying nanomolar activity against MMP-12 and which was co-crystallized with MMP-12.

PMID:
16002291
DOI:
10.1016/j.bmcl.2005.05.079
[Indexed for MEDLINE]

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