Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: A class of potent aggrecanase-1 inhibitors

Autor:	Darrin William Hopper, Elisabeth A. Morris, David Brian How, Manus Ipek, Erica Reifenberg, Phaik-Eng Sum, Matthew D. Vera, Eric Feyfant, Katy E. Georgiadis, Jerauld S. Skotnicki, Manas K. Majumdar, Jennifer R. Thomason, Qin Wang, Joshua James Sabatini, Cristin C. Keohan, Richard Sheldon, Jason Shaoyun Xiang, Yonghan Hu
Rok vydání:	2009
Předmět:	Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Cartilage metabolism Biochemistry Chemical synthesis Inhibitory Concentration 50 Matrix Metalloproteinase 13 Osteoarthritis Drug Discovery medicine Humans Molecular Biology Aggrecan Aggrecanase chemistry.chemical_classification Sulfonamides Chemistry Cartilage Organic Chemistry Biological activity ADAMTS4 Protein ADAM Proteins Enzyme medicine.anatomical_structure Models Chemical Drug Design Matrix Metalloproteinase 2 Molecular Medicine Proteoglycans Procollagen N-Endopeptidase
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:2487-2491
ISSN:	0960-894X
Popis:	The prevention of aggrecan (a key component of cartilage) cleavage via the inhibition of aggrecanase-1 may provide a unique opportunity to stop the progression of cartilage degradation in osteoarthritis. The evaluation of a series of biphenylsulfonamides resulted in the identification of the ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides analogs (19-21 and 24) with improved Agg-1 inhibition and MMP-2, MMP-13 activity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bfdd5fb1dbd1d63aa8e94dff08e3143 https://doi.org/10.1016/j.bmcl.2009.03.056 Zobrazit plný text záznamu Full Text from ScienceDirect