2. Academic Validation
  3. Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase

Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase

  • Bioorg Med Chem Lett. 1998 Apr 21;8(8):897-902. doi: 10.1016/s0960-894x(98)00142-5.
A Y Jeng 1,  M Chou,  D T Parker
Affiliations

Affiliation

  • 1 Metabolic and Cardiovascular Diseases Research, Novartis Pharmaceuticals, Summit, NJ 07901, USA.
PMID: 9871508 DOI: 10.1016/s0960-894x(98)00142-5
Abstract

The structural requirements of sulfonamide-based hydroxamic acid 1 for inhibition of macrophage metalloelastase (MME) were investigated. A short aliphatic group at the R2 position together with an aromatic group at the R3 position significantly improved the inhibitory activity. Compounds 32, 34, and 40 were the most potent inhibitors of MME with IC50 values between 5 and 6 nM.

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