Molecules (2017)
Update date:2022-08-03
Topics:
Wang, Xinran
Lin, Xuehua
Xu, Xuanqi
Li, Wei
Hao, Lijuan
Liu, Chunchi
Zhao, Dongmei
Cheng, Maosheng
Cholesteryl ester transfer protein (CETP) has been identified as a potential target for cardiovascular disease (CVD) for its important role in the reverse cholesteryl transfer (RCT) process. In our previous work, compound 5 was discovered as a moderate CETP inhibitor. The replacement of the amide linker by heterocyclic aromatics and then a series of N,N-substituted-4-arylthiazole-2-methylamine derivatives were designed by utilizing a conformational restriction strategy. Thirty-six compounds were synthesized and evaluated for their CETP inhibitory activities. Structure-activity relationship studies indicate that electron donor groups substituted ring A, and electron-withdrawing groups at the 4-position of ring B were critical for potency. Among these compounds, compound 30 exhibited excellent CETP inhibitory activity (IC50 = 0.79 ± 0.02 μM) in vitro and showed an acceptable metabolic stability.
View MoreSuzhou Jingye Medicine & Chemical Co., Ltd
website:http://www.jingyechem.cn
Contact:+86-512-66658588
Address:No. 88, Sanlian Street, Jinfeng Road, Suzhou New District, Jiangsu Province, P. R. China
Contact:+1-973-357-0577
Address:10 Taft Rd.
Shanghai Sungo Technology Chemical Co., Ltd
Contact:0086-21-51385579
Address:Room2010, F/20, Tonghua Plaza, NO 345 Jinxiang Road, Jinqiao Export Processing Zone, Shanghai, 201206 P.R.CHINA
Shanghai Sunway Pharmaceutical Technology Co.,Ltd.
Contact:+86-21-5161 3915
Address:Shanghai YangPu
Qingdao XinYongAn Chemicals Co., Ltd
Contact:+86-532-81107967
Address:Chengyang dual-port industrial park by the sea,Qingdao
Doi:10.1021/jo00891a003
(1975)Doi:10.1039/c39740000323
(1974)Doi:10.1002/ejoc.202000823
(2020)Doi:10.1023/B:RUGC.0000016002.83302.af
(2003)Doi:10.1557/mrs2001.93
(1938)Doi:10.1021/jm00255a018
(1974)