5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
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DOI：
10.1016/j.bmcl.2006.12.020
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发表时间：
2007-03-01
影响因子：
2.7
通讯作者：
Morris, Elisabeth A.
中科院分区：
文献类型：
--
作者：
Gilbert, Adam M.;Bursavich, Matthew G.;Morris, Elisabeth A.
描述了一系列的5-（（1h -吡唑-4-酰基）亚甲基）-2-硫氧噻唑烷-4- 1抑制剂ADAMTS-5（聚集酶-2）。这些化合物显示出对ADAMTS-5的mu - M功能抑制，代表了一类具有抑制聚集蛋白降解潜力的新药物，聚集蛋白是骨质疏松症中软骨丢失的主要成分。值得注意的是，化合物12具有ADAMTS-5的IC50: 1.1 μ M，比ADAMTS-4 （aggrcanase -1）具有40倍的功能选择性。(c) 2006 Elsevier Ltd.版权所有。
A series of 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5 (aggrecanase-2) is described. These compounds show mu M functional inhibition of ADAMTS-5, and represent a new class of agents with the potential of inhibiting degradation of aggrecan, a major component of cartilage which is lost in osteoporosis. Compound 12 is noteworthy in that it has an ADAMTS-5 IC50: 1.1 mu M and shows > 40-fold functional selectivity over ADAMTS-4 (aggrecanase-1). (c) 2006 Elsevier Ltd. All rights reserved.