TY - JOUR
T1 - Synthesis of a novel series of imidazo[1,2-α]pyridines as acyl-CoA
T2 - Cholesterol acyltransferase (ACAT) inhibitors
AU - Jin, Yinglan
AU - Rho, Mun Chual
AU - Gajulapati, Kondaji
AU - Jung, Hwa Young
AU - Boovanahalli, Shanthaveerappa K.
AU - Lee, Jee Hyun
AU - Song, Gyu Yong
AU - Choi, Jung Ho
AU - Kim, Young Kook
AU - Lee, Kyeong
AU - Choi, Yongseok
PY - 2009/6
Y1 - 2009/6
N2 - 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.
AB - 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.
KW - Acyl CoA: cholestrol acyl transferase (ACAT)
KW - HepG2 cells
KW - Imidazo[1,2-α]pyridines
KW - Structure-activity relationship
UR - http://www.scopus.com/inward/record.url?scp=69249186403&partnerID=8YFLogxK
U2 - 10.5012/bkcs.2009.30.6.1297
DO - 10.5012/bkcs.2009.30.6.1297
M3 - Article
AN - SCOPUS:69249186403
SN - 0253-2964
VL - 30
SP - 1297
EP - 1304
JO - Bulletin of the Korean Chemical Society
JF - Bulletin of the Korean Chemical Society
IS - 6
ER -