Potent, selective, and orally bioavailable matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis

Autor:	Wei Li, Qin Wang, Jason Shaoyun Xiang, Jeremy I. Levin, Leif M. Laakso, Xuemei Du, Thomas S. Rush, Jennifer R. Thomason, Manus Ipek, Tam Steve Yik-Kai, Yonghan Hu, Jerauld S. Skotnicki, Jean Schmid, Martin J. DiGrandi, Jianchang Li
Rok vydání:	2005
Předmět:	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
Zdroj:	Bioorganic & Medicinal Chemistry. 13:6629-6644
ISSN:	0968-0896
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22d053419b0d61b6ff86d04a32ae1868 https://doi.org/10.1016/j.bmc.2005.07.076 Zobrazit plný text záznamu Full Text from ScienceDirect