选择性非锌结合 MMP13 抑制剂的先导优化。第 2 部分。
Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.
机构信息
Respiratory and Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield SK10 4TG, UK.
出版信息
Bioorg Med Chem Lett. 2012 Jan 1;22(1):271-7. doi: 10.1016/j.bmcl.2011.11.034. Epub 2011 Nov 16.
PMID:22153941
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.
摘要
定向筛选已鉴定出一系列新型非锌结合 MMP13 抑制剂，它们具有良好的活性，同时对相关 MMP 具有优异的选择性。一个先导化合物优化研究项目提供了具有增强的 MMP13 效力、良好的选择性和可接受的生物利用度特征的化合物，这导致在人体内预测的每天两次给药方案。
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