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Identification of potent and selective MMP-13 inhibitors.

Abstract：

:A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 microM) inhibitor that did not bear a zinc chelator. Structure-based drug design strategies were employed to append a Zn-chelating group to one end of the molecule and functionality to enhance selectivity to the other. A compound from this series demonstrated rat oral bioavailability and efficacy in a bovine articular cartilage explant model.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wu J,Rush TS 3rd,Hotchandani R,Du X,Geck M,Collins E,Xu ZB,Skotnicki J,Levin JI,Lovering FE

doi

10.1016/j.bmcl.2005.06.019

subject

Has Abstract

pub_date

2005-09-15 00:00:00

pages

4105-9

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00776-6

journal_volume

15

pub_type

杂志文章

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