Synthesis of a novel series of imidazo[1,2-α]pyridines as Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors

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Title
Synthesis of a novel series of imidazo[1,2-α]pyridines as Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors
Author(s)
Y Jin; Mun Chual Rho; K Gajulapati; H Y Jung; S K Boovanahalli; J H Lee; G Y Song; J H Choi; Young Kook Kim; Kyeong Lee; Y Choi
Bibliographic Citation
Bulletin of Korean Chemical Society, vol. 30, no. 6, pp. 1297-1304
Publication Year
2009
Abstract
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.
Keyword
imidazo[1,2-α]pyridines, acyl CoAcholestrol acyl transferase (ACAT)HepG2 cells, structure-activity relationship
ISSN
0253-2964
Publisher
Wiley
DOI
http://dx.doi.org/10.5012/bkcs.2009.30.6.1297
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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