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

[摘要]：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. (C) 2009 Elsevier Ltd. All rights reserved.

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