School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264003, China.
Bioorg Med Chem. 2020 Oct 1;28(19):115683. doi: 10.1016/j.bmc.2020.115683. Epub 2020 Aug 3.
A series of 4-aryl-5-aminoalkyl-thiazole-2-amines were designed and synthesized, and their inhibitory activity on ROCK II was screened by enzyme-linked immunosorbent assay (ELISA). The results showed that 4-aryl-5-aminomethyl-thiazole-2-amines derivatives had certain ROCK II inhibitory activities. Compound 10l showed ROCK II inhibitory activity with IC value of 20 nM.
设计并合成了一系列 4-芳基-5-氨烷基噻唑-2-胺，通过酶联免疫吸附测定（ELISA）筛选其对 ROCK II 的抑制活性。结果表明，4-芳基-5-氨甲基噻唑-2-胺衍生物具有一定的 ROCK II 抑制活性。化合物 10l 对 ROCK II 的抑制活性的 IC 值为 20 nM。
