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ID: ALA1938343

Journal: Bioorg Med Chem Lett

Title: Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.

Authors: De Savi C, Morley AD, Nash I, Karoutchi G, Page K, Ting A, Gerhardt S.

Abstract: Directed screening has identified a novel series of non-zinc binding MMP13 inhibitors that possess good levels of activity whilst demonstrating excellent selectivity over related MMPs. A lead optimisation campaign has delivered compounds with enhanced MMP13 potency, good selectivity and acceptable bioavailability profiles leading to a predicted twice-a-day dosing regimen in man.

CiteXplore: 22153941

DOI: 10.1016/j.bmcl.2011.11.034