一系列含有噻唑烷-4-酮的噻唑衍生物，作为非竞争性 ADAMTS-5（聚集素酶-2）抑制剂。
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.
机构信息
Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan.
出版信息
Bioorg Med Chem Lett. 2013 Apr 1;23(7):2106-10. doi: 10.1016/j.bmcl.2013.01.121. Epub 2013 Feb 9.
PMID:23453070
Abstract
A series of thiazole bearing thiazolidin-4-one was discovered via high-throughput screening as non-competitive inhibitors of ADAMTS-5. Compound 31 appeared to give the best ADAMTS-5 inhibition and good selectivity over other metalloproteases.
摘要
通过高通量筛选，发现了一系列含有噻唑的噻唑烷-4-酮类化合物，它们是非竞争性的 ADAMTS-5 抑制剂。化合物 31 似乎对 ADAMTS-5 有最好的抑制作用，并且对其他金属蛋白酶具有良好的选择性。
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