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

  • Jin, Yinglan
  • Rho, Mun-Chual
  • Gajulapati, Kondaji
  • Jung, Hwa Young
  • Boovanahalli, Shanthaveerappa K.
  • ... Choi, Yongseok
  • 외 5명
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초록

A novel series of imidazo[1,2-alpha]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.

키워드

Imidazo[1,2-alpha]pyridinesAcyl CoA: cholestrol acyl transferase (ACAT)HepG2 cellsStructure-activity relationshipSAUCERNEOL-BDERIVATIVESMETABOLISMABSORPTIONAGENTS
제목
Synthesis of a Novel Series of Imidazo[1,2-alpha]pyridines as Acyl-CoA: Cholesterol Acyltransferase (ACAT) Inhibitors
저자
Jin, YinglanRho, Mun-ChualGajulapati, KondajiJung, Hwa YoungBoovanahalli, Shanthaveerappa K.Lee, Jee HyunSong, Gyu-YongChoi, Jung HoKim, Young KookLee, KyeongChoi, Yongseok
발행일
2009-06-20
유형
Article
저널명
Bulletin of the Korean Chemical Society
30
6
페이지
1297 ~ 1304