MMP-13 selective alpha-sulfone hydroxamates: Identification of selective P1′ amides

Autor:	James R. Kiefer, Barta Thomas E, Heintz Robert M, Yvette M. Fobian, Daniel P. Becker, Grace E. Munie, Patrick B. Mullins, John M. Molyneaux, Brent V. Mischke, Darren J. Kassab, Louis J. Bedell, John N. Freskos
Rok vydání:	2011
Předmět:	medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Ether Carboxamide Matrix Metalloproteinase Inhibitors Hydroxamic Acids Biochemistry Chemical synthesis Substrate Specificity Sulfone Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Amide Drug Discovery medicine Humans Structure–activity relationship Protease Inhibitors Molecular Biology Hydroxamic acid Molecular Structure Organic Chemistry Amides chemistry Molecular Medicine Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:2823-2825
ISSN:	0960-894X
Popis:	Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we report on a series of hydroxamic acids with a flexible amide P1' substituents. We identify an amide which spares both MMP-1 and -14, and shows >500 fold selectivity for MMP-13 versus MMP-2 and -8.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d64fc828c6eacfa443f80cdc71c9f154 https://doi.org/10.1016/j.bmcl.2011.03.095 Zobrazit plný text záznamu Full Text from ScienceDirect