Research Article Details

Article ID: A34957
PMID: 22153941
Source: Bioorg Med Chem Lett
Title: Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.
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.
DOI: 10.1016/j.bmcl.2011.11.034