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Potent, selective, and orally bioavailable matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis |
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| Authors: | Hu Yonghan Xiang Jason S DiGrandi Martin J Du Xuemei Ipek Manus Laakso Leif M Li Jianchang Li Wei Rush Thomas S Schmid Jean Skotnicki Jerauld S Tam Steve Thomason Jennifer R Wang Qin Levin Jeremy I |
| Affiliation: | aDepartment of Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, MA 02140, USA bDepartment of Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA cDepartment of Drug Safety and Metabolism, Wyeth Research, 1 Burtt Road, Andover, MA 01810, USA |
| Abstract: | Modification of -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. |
| Keywords: | MMP-13 inhibitor Biphenylsulfonamide carboxylate Benzofuran Osteoarthritis |
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