Bioorganic & medicinal chemistry, 2005-12, Vol.13 (24), p.6629-6644
2005
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Potent, selective, and orally bioavailable matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis
- Ist Teil von
- Bioorganic & medicinal chemistry, 2005-12, Vol.13 (24), p.6629-6644
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2005
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Modification of α-biphenylsulfonamidocarboxylic acids led to potent and selective MMP-13 inhibitors. Compound 16 showed 100% oral bioavailability in rats and demonstrated >50% inhibition of bovine cartilage degradation at 10 ng/mL. Modification of α-biphenylsulfonamidocarboxylic acids led to potent and selective MMP-13 inhibitors. Compound 16 showed 100% oral bioavailability in rats and demonstrated >50% inhibition of bovine cartilage degradation at 10 ng/mL.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0968-0896eISSN: 1464-3391DOI: 10.1016/j.bmc.2005.07.076Titel-ID: cdi_crossref_primary_10_1016_j_bmc_2005_07_076
- Format
- –
- Schlagworte
- Administration, Oral, Animals, Benzofuran, Benzofurans - chemical synthesis, Benzofurans - chemistry, Biological and medical sciences, Biphenylsulfonamide carboxylate, Bones, joints and connective tissue. Antiinflammatory agents, Collagenases - chemistry, Collagenases - metabolism, Drug Evaluation, Preclinical, Enzyme Inhibitors - administration & dosage, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacokinetics, Enzyme Inhibitors - pharmacology, Inhibitory Concentration 50, Matrix Metalloproteinase 13, Matrix Metalloproteinase Inhibitors, Medical sciences, MMP-13 inhibitor, Models, Molecular, Molecular Structure, Osteoarthritis, Osteoarthritis - drug therapy, Pharmacology. Drug treatments, Rats, Substrate Specificity