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 Pharmacy

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

2 Scopus citations

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
State	Published - 20 Feb 2015

Keywords

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

UN SDGs

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

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10.1002/bkcs.10123

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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",

author = "Minkyoung Kim and Jinsun Kwon and Kim, {Mun Ock} and Sarbjit Singh and Kim, {Sang Kyum} and Kyeong Lee and Kiho Lee and Lee, {Hyun Sun} and Yongseok Choi",

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doi = "10.1002/bkcs.10123",

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T1 - Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors

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

SP - 628

EP - 635

JO - Bulletin of the Korean Chemical Society

JF - Bulletin of the Korean Chemical Society

IS - 2

ER -

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

Abstract

Keywords

UN SDGs

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