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

Research output: Contribution to journalArticle

20 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1297-1304
Number of pages8
JournalBulletin of the Korean Chemical Society
Volume30
Issue number6
DOIs
Publication statusPublished - 2009 Jun 1

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Sterol O-Acyltransferase
Pyridines
Cholesterol Esters

Keywords

  • Acyl CoA: cholestrol acyl transferase (ACAT)
  • HepG2 cells
  • Imidazo[1,2-α]pyridines
  • Structure-activity relationship

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Synthesis of a novel series of imidazo[1,2-α]pyridines as acyl-CoA : Cholesterol acyltransferase (ACAT) inhibitors. / Jin, Yinglan; Rho, Mun Chual; Gajulapati, Kondaji; Jung, Hwa Young; Boovanahalli, Shanthaveerappa K.; Lee, Jee Hyun; Song, Gyu Yong; Choi, Jung Ho; Kim, Young Kook; Lee, Kyeong; Choi, Yongseok.

In: Bulletin of the Korean Chemical Society, Vol. 30, No. 6, 01.06.2009, p. 1297-1304.

Research output: Contribution to journalArticle

Jin, Y, Rho, MC, Gajulapati, K, Jung, HY, Boovanahalli, SK, Lee, JH, Song, GY, Choi, JH, Kim, YK, Lee, K & Choi, Y 2009, 'Synthesis of a novel series of imidazo[1,2-α]pyridines as acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors', Bulletin of the Korean Chemical Society, vol. 30, no. 6, pp. 1297-1304. https://doi.org/10.5012/bkcs.2009.30.6.1297
Jin, Yinglan ; Rho, Mun Chual ; Gajulapati, Kondaji ; Jung, Hwa Young ; Boovanahalli, Shanthaveerappa K. ; Lee, Jee Hyun ; Song, Gyu Yong ; Choi, Jung Ho ; Kim, Young Kook ; Lee, Kyeong ; Choi, Yongseok. / Synthesis of a novel series of imidazo[1,2-α]pyridines as acyl-CoA : Cholesterol acyltransferase (ACAT) inhibitors. In: Bulletin of the Korean Chemical Society. 2009 ; Vol. 30, No. 6. pp. 1297-1304.
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