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The design and synthesis of aryl hydroxamic acid inhibitors of MMPs and TACE
- Source :
- Current topics in medicinal chemistry. 4(12)
- Publication Year :
- 2004
-
Abstract
- Three different classes of aryl hydroxamic acid scaffolds have been explored and provided potent inhibitors of MMP-1, -2, -9, -13 and TACE. Structure-based design has allowed the evolution of these inhibitors from broad spectrum inhibitors into compounds that are more selective for MMPs relevant to particular disease states. Aryl hydroxamates selective for MMP-9, MMP-13 and TACE have been disclosed that may aid in the study of the physiological role of these enzymes. Furthermore, the different selectivity profiles offered by these MMP/TACE inhibitors may allow the determination of which metalloprotease, or group of metalloproteases, must be inhibited for the safe, long-term treatment of osteoarthritis, rheumatoid arthritis and cancer. Some of these compounds have demonstrated useful biological activity in efficacy models relevant to osteoarthritis and rheumatoid arthritis and are therefore potential clinical candidates.
- Subjects :
- Stereochemistry
Matrix metalloproteinase inhibitor
Osteoarthritis
Matrix metalloproteinase
Pharmacology
ADAM17 Protein
Matrix Metalloproteinase Inhibitors
Hydroxamic Acids
chemistry.chemical_compound
Drug Discovery
medicine
Animals
Humans
Protease Inhibitors
chemistry.chemical_classification
Metalloproteinase
Hydroxamic acid
Aryl
Metalloendopeptidases
Biological activity
General Medicine
medicine.disease
ADAM Proteins
Enzyme
chemistry
Rheumatoid arthritis
Drug Design
Subjects
Details
- ISSN :
- 15680266
- Volume :
- 4
- Issue :
- 12
- Database :
- OpenAIRE
- Journal :
- Current topics in medicinal chemistry
- Accession number :
- edsair.doi.dedup.....29fad08be073d0671fac0dd3655d2254