Selective Inhibition of Matrix Metalloproteinase Isozymes and in Vivo Protection Against Emphysema by Substituted Gamma-keto Carboxylic Acids.
From: State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China. madw@mail.sioc.ac.cn
Journal of medicinal chemistry
- Publish Date: Jan 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 2
- Pages: 456-8
- Medium: Print
- Language: English
- Citation (JAMA): Ma Dawei, Jiang Yongwen, Chen Fangping, et al. Selective Inhibition of Matrix Metalloproteinase Isozymes and in Vivo Protection Against Emphysema by Substituted Gamma-keto Carboxylic Acids.. J. Med. Chem. Jan 2006;49:456-8
Abstract
The synthesis and matrix metalloproteinase (MMP) inhibitory activity of a series of gamma-keto carboxylic acids are described. Among nine MMP isozymes tested, compound 1j displays selective inhibition of MMP-2, -9, and -12 with IC(50) values between 0.20 and 1.51 microuM, and in male golden Syrian hamsters, it shows protection against PPE-induced emphysema.
Mesh Headings (Keywords): Animals, Cricetinae, Isoenzymes, Keto Acids, Male, Matrix Metalloproteinases, Mesocricetus, Models, Molecular, Pancreatic Elastase, Pulmonary Emphysema, Structure-Activity Relationship, Swine
Check for Full Text / PubMed Unique Identifier (PMID): 16420030
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