2. Academic Validation
  3. A novel series of highly selective inhibitors of MMP-3

A novel series of highly selective inhibitors of MMP-3

  • Bioorg Med Chem Lett. 2007 Dec 15;17(24):6750-3. doi: 10.1016/j.bmcl.2007.10.042.
Gavin A Whitlock 1,  Kevin N Dack,  Roger P Dickinson,  Mark L Lewis
Affiliations

Affiliation

  • 1 Sandwich Chemistry Department, Pfizer Global Research and Development, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. gavin.whitlock@pfizer.com
PMID: 18029177 DOI: 10.1016/j.bmcl.2007.10.042
Abstract

The design and synthesis of a series of highly selective hydroxamate inhibitors of stromelysin-1 (MMP-3) is described. Substitution of a 4-biaryl piperidine sulfonamide core, which binds at the S1' subsite of MMP-3, was optimised to give potent inhibitors of MMP-3, with greater than 300-fold selectivity over MMP-1, MMP-2, MMP-9 and MMP-14. Compounds 26 and 27 were identified as having the best balance of pharmacology and properties required for topical Drug Delivery.

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