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Potent, selective, and orally bioavailable matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis
- Source :
- Bioorganic & Medicinal Chemistry. 13:6629-6644
- Publication Year :
- 2005
- Publisher :
- Elsevier BV, 2005.
-
Abstract
- Modification of alpha-biphenylsulfonamidocarboxylic acids led to potent and selective MMP-13 inhibitors. Compound 16 showed 100% oral bioavailability in rats and demonstrated50% inhibition of bovine cartilage degradation at 10 ng/mL.
- Subjects :
- Models, Molecular
Clinical Biochemistry
Drug Evaluation, Preclinical
Administration, Oral
Pharmaceutical Science
Osteoarthritis
Matrix Metalloproteinase Inhibitors
Matrix metalloproteinase
Pharmacology
Biochemistry
Substrate Specificity
Inhibitory Concentration 50
Pharmacokinetics
Oral administration
Matrix Metalloproteinase 13
Drug Discovery
medicine
Animals
Collagenases
Enzyme Inhibitors
Molecular Biology
Benzofurans
chemistry.chemical_classification
Molecular Structure
biology
Organic Chemistry
medicine.disease
Bovine Cartilage
Rats
Bioavailability
Enzyme
chemistry
Enzyme inhibitor
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....22d053419b0d61b6ff86d04a32ae1868