Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors

Minkyoung Kim; Jinsun Kwon; Mun Ock Kim; Sarbjit Singh; Sang Kyum Kim; Kyeong Lee; Kiho Lee; Hyun Sun Lee; Yongseok Choi

doi:10.1002/bkcs.10123

Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors

Minkyoung Kim, Jinsun Kwon, Mun Ock Kim, Sarbjit Singh, Sang Kyum Kim, Kyeong Lee, Kiho Lee, Hyun Sun Lee, Yongseok Choi

Department of Biotechnology

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

2 Citations (Scopus)

Abstract

A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds 8u and 8v exhibited selective and potent DGAT-1 inhibitory activities. In addition, compound 8u dose-dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound 8u for an oral lipid tolerance test showed a significant decrease in plasma triglyceride levels compared with vehicle-treated control animals, indicating delayed absorption of triglyceride after an acute lipid challenge.

Original language	English
Pages (from-to)	628-635
Number of pages	8
Journal	Bulletin of the Korean Chemical Society
Volume	36
Issue number	2
DOIs	https://doi.org/10.1002/bkcs.10123
Publication status	Published - 2015 Feb 20

Bibliographical note

Publisher Copyright:
© 2015 Korean Chemical Society, Seoul & Wiley-VCH Verlag GmbH & Co. KGaA.

Keywords

Diacylglycerol O-acyltransferase
Diacylglycerol O-acyltransferase inhibitor
Hydrazide
Obesity
Triglyceride

ASJC Scopus subject areas

General Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/bkcs.10123

Cite this

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title = "Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors",

abstract = "A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds 8u and 8v exhibited selective and potent DGAT-1 inhibitory activities. In addition, compound 8u dose-dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound 8u for an oral lipid tolerance test showed a significant decrease in plasma triglyceride levels compared with vehicle-treated control animals, indicating delayed absorption of triglyceride after an acute lipid challenge.",

keywords = "Diacylglycerol O-acyltransferase, Diacylglycerol O-acyltransferase inhibitor, Hydrazide, Obesity, Triglyceride",

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AU - Kim, Minkyoung

AU - Kwon, Jinsun

AU - Kim, Mun Ock

AU - Singh, Sarbjit

AU - Kim, Sang Kyum

AU - Lee, Kyeong

AU - Lee, Kiho

AU - Lee, Hyun Sun

AU - Choi, Yongseok

PY - 2015/2/20

Y1 - 2015/2/20

N2 - A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds 8u and 8v exhibited selective and potent DGAT-1 inhibitory activities. In addition, compound 8u dose-dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound 8u for an oral lipid tolerance test showed a significant decrease in plasma triglyceride levels compared with vehicle-treated control animals, indicating delayed absorption of triglyceride after an acute lipid challenge.

AB - A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds 8u and 8v exhibited selective and potent DGAT-1 inhibitory activities. In addition, compound 8u dose-dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound 8u for an oral lipid tolerance test showed a significant decrease in plasma triglyceride levels compared with vehicle-treated control animals, indicating delayed absorption of triglyceride after an acute lipid challenge.

KW - Diacylglycerol O-acyltransferase

KW - Diacylglycerol O-acyltransferase inhibitor

KW - Hydrazide

KW - Obesity

KW - Triglyceride

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VL - 36

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IS - 2

ER -

Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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