Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors

Kyeong Lee; Minkyoung Kim; Boah Lee; Jail Goo; Jiyoung Kim; Ravi Naik; Jee Hee Seo; Mun Ock Kim; Youngjoo Byun; Gyu Yong Song; Hyun Sun Lee; Yongseok Choi

doi:10.1039/c2ob27114a

Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors

Kyeong Lee, Minkyoung Kim, Boah Lee, Jail Goo, Jiyoung Kim, Ravi Naik, Jee Hee Seo, Mun Ock Kim, Youngjoo Byun, Gyu Yong Song, Hyun Sun Lee, Yongseok Choi

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

A series of indolyl acrylamide derivatives was synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Furfurylamine containing indolyl acrylamide derivative 5h exhibited the most potent DGAT inhibitory activity using microsomes prepared from rat liver. Further evaluation against human DGAT-1 and DGAT-2 identified indolyl acrylamide analogues as selective inhibitors against human DGAT-2. In addition, the most potent compound 5h inhibited triglyceride synthesis dose-dependently in HepG2 cell lines.

Original language	English (US)
Pages (from-to)	849-858
Number of pages	10
Journal	Organic and Biomolecular Chemistry
Volume	11
Issue number	5
DOIs	https://doi.org/10.1039/c2ob27114a
State	Published - Feb 7 2013
Externally published	Yes

ASJC Scopus subject areas

Physical and Theoretical Chemistry
Organic Chemistry
Biochemistry

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title = "Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors",

abstract = "A series of indolyl acrylamide derivatives was synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Furfurylamine containing indolyl acrylamide derivative 5h exhibited the most potent DGAT inhibitory activity using microsomes prepared from rat liver. Further evaluation against human DGAT-1 and DGAT-2 identified indolyl acrylamide analogues as selective inhibitors against human DGAT-2. In addition, the most potent compound 5h inhibited triglyceride synthesis dose-dependently in HepG2 cell lines.",

author = "Kyeong Lee and Minkyoung Kim and Boah Lee and Jail Goo and Jiyoung Kim and Ravi Naik and Seo, {Jee Hee} and Kim, {Mun Ock} and Youngjoo Byun and Song, {Gyu Yong} and Lee, {Hyun Sun} and Yongseok Choi",

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doi = "10.1039/c2ob27114a",

language = "English (US)",

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TY - JOUR

T1 - Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors

AU - Lee, Kyeong

AU - Kim, Minkyoung

AU - Lee, Boah

AU - Goo, Jail

AU - Kim, Jiyoung

AU - Naik, Ravi

AU - Seo, Jee Hee

AU - Kim, Mun Ock

AU - Byun, Youngjoo

AU - Song, Gyu Yong

AU - Lee, Hyun Sun

AU - Choi, Yongseok

PY - 2013/2/7

Y1 - 2013/2/7

N2 - A series of indolyl acrylamide derivatives was synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Furfurylamine containing indolyl acrylamide derivative 5h exhibited the most potent DGAT inhibitory activity using microsomes prepared from rat liver. Further evaluation against human DGAT-1 and DGAT-2 identified indolyl acrylamide analogues as selective inhibitors against human DGAT-2. In addition, the most potent compound 5h inhibited triglyceride synthesis dose-dependently in HepG2 cell lines.

AB - A series of indolyl acrylamide derivatives was synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Furfurylamine containing indolyl acrylamide derivative 5h exhibited the most potent DGAT inhibitory activity using microsomes prepared from rat liver. Further evaluation against human DGAT-1 and DGAT-2 identified indolyl acrylamide analogues as selective inhibitors against human DGAT-2. In addition, the most potent compound 5h inhibited triglyceride synthesis dose-dependently in HepG2 cell lines.

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DO - 10.1039/c2ob27114a

M3 - Article

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AN - SCOPUS:84872066369

SN - 1477-0520

VL - 11

SP - 849

EP - 858

JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

IS - 5

ER -

Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors

Abstract

ASJC Scopus subject areas

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