Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective α-sulfone hydroxamates

Autor:	Jeffery N. Carroll, Craig Swearingen, Decrescenzo Gary A, Rico Joseph G, Theresa R. Fletcher, Daniel P. Becker, Joseph J. McDonald, Susan L. Hockerman, Grace E. Munie, Stephen A. Kolodziej, Boehm Terri L, Debbie A. Mischke, Nathan W. Stehle
Rok vydání:	2010
Předmět:	Stereochemistry Matrix metalloproteinase inhibitor Clinical Biochemistry Administration Oral Biological Availability Pharmaceutical Science Matrix Metalloproteinase Inhibitors Hydroxamic Acids Biochemistry Chemical synthesis Substrate Specificity Sulfone Small Molecule Libraries chemistry.chemical_compound Piperidines Oral administration Drug Discovery Matrix Metalloproteinase 14 Animals Sulfones Molecular Biology Hydroxamic acid biology Organic Chemistry Biological activity Rats Bioavailability Solubility chemistry Enzyme inhibitor biology.protein Molecular Medicine Matrix Metalloproteinase 1
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:3557-3560
ISSN:	0960-894X
Popis:	A series of phenyl piperidine alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b61c5bde65513f60ea0896cfb24e7ec https://doi.org/10.1016/j.bmcl.2010.04.130 Zobrazit plný text záznamu Full Text from ScienceDirect