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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 30, Number 6
BKCSDE 30(6)
June 20, 2009 

Synthesis of a Novel Series of Imidazo[1,2-α]pyridines as Acyl-CoA: Cholesterol Acyltransferase (ACAT) Inhibitors
Yinglan Jin, Mun Chual Rho, Kondaji Gajulapati, Hwa Young Jung, Shanthaveerappa K Boovanahalli, Jee Hyun Lee, Gyu Yong Song, Jung Ho Choi, Young Kook Kim, Kyeong Lee*, Yongseok Choi*
Imidazo[1,2-α]pyridines, Acyl CoA: cholestrol acyl transferase (ACAT), HepG2 cells, Structure-activity relationship
A novel series of imidazo[1,2-α]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.
1297 - 1304
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