Document Report Card

Basic Information

ID: ALA1153501

Journal: Bioorg Med Chem Lett

Title: 3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding.

Authors: Li W, Hu Y, Li J, Thomason JR, DeVincentis D, Du X, Wu J, Hotchandani R, Rush TS, Skotnicki JS, Tam S, Chockalingam PS, Morris EA, Levin JI.

Abstract: Potent 3,4-disubstituted benzofuran P1' MMP-13 inhibitors have been prepared. Selectivity over MMP-2 was achieved through a substituent at the C4 position of the benzofuran P1' moiety of the molecule. By replacing a backbone benzene with a pyridine and valine with threonine, compounds (e.g., 44) with greatly reduced plasma protein binding were also obtained.

CiteXplore: 19625186

DOI: 10.1016/j.bmcl.2009.07.008