Synthesis of a Novel Series of Imidazo[1,2-¥á]pyridines as Acyl-CoA: Cholesterol Acyltransferase (ACAT) Inhibitors

Bulletin of the Korean chemical society

Gyu Yong Song¹  Young Kook Kim¹  Jung Ho Choi¹  Yongseok Choi¹  Kondaji Gajulapati¹  Shanthaveerappa K Boovanahalli¹  Yinglan Jin¹  Hwa Young Jung¹  Kyeong Lee¹  Mun Chual Rho¹  Jee Hyun Lee¹ 

关键词: Imidazo[1;    2-¥á]pyridines;    Acyl CoA: cholestrol acyl transferase (ACAT);    HepG2 cells;    Structure-activity relationship;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A novel series of imidazo[1,2-メ]pyridines was designed, synthesized, and tested for their ability to inhibit acyl-CoA:cholesterol acyltransferase. Preliminary lead optimization efforts resulted in the identification of ACAT inhibitors represented by analogues 5b, 5c, 6a, 6c, 7b, and 7c. The ACAT inhibitory activity of these compounds was further established by potent inhibition of cholesteryl ester formation in HepG2 cells by a representative analogue 7b.

【 授权许可】

Unknown