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http://dx.doi.org/10.5012/bkcs.2009.30.6.1297

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

Jin, Ying-Lan (Korea Research Institute of Biosciences and Biotechnology (KRIBB))
Rho, Mun-Chual (Korea Research Institute of Biosciences and Biotechnology (KRIBB))
Gajulapati, Kondaji (School of Life Sciences and Biotechnology, Korea University)
Jung, Hwa-Young (School of Life Sciences and Biotechnology, Korea University)
Boovanahalli, Shanthaveerappa K. (Korea Research Institute of Biosciences and Biotechnology (KRIBB))
Lee, Jee-Hyun (College of Pharmacy, Chungnam National University)
Song, Gyu-Yong (College of Pharmacy, Chungnam National University)
Choi, Jung-Ho (Korea Research Institute of Biosciences and Biotechnology (KRIBB))
Kim, Young-Kook (Korea Research Institute of Biosciences and Biotechnology (KRIBB))
Lee, Kyeong (Korea Research Institute of Biosciences and Biotechnology (KRIBB))
Choi, Yong-Seok (School of Life Sciences and Biotechnology, Korea University)
Publication Information
Bulletin of the Korean Chemical Society / v.30, no.6, 2009 , pp. 1297-1304 More about this Journal
Abstract
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.
Keywords
Imidazo[1,2-$\alpha$]pyridines; Acyl CoA: cholestrol acyl transferase (ACAT); HepG2 cells; Structure-activity relationship;
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