Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists

Eunkyung Kim; Chan Sun Park; Taedong Han; Myung Ho Bae; Wonee Chong; Choong Hyun Lee; Young Ah Shin; Byung Nak Ahn; Mi Kyung Kim; Chang Yell Shin; Moon Ho Son; Jin Kwan Kim; Ho Sang Moon; Hyun Joo Shim; Eun Jung Kim; Soon Hoe Kim; Joong In Lim; Chun Ho Lee

doi:10.1016/j.bmcl.2008.08.020

Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists

Eunkyung Kim
, Chan Sun Park
, Taedong Han
, Myung Ho Bae
, Wonee Chong
, Choong Hyun Lee^*
, Young Ah Shin
, Byung Nak Ahn
, Mi Kyung Kim
, Chang Yell Shin
, Moon Ho Son
, Jin Kwan Kim
, Ho Sang Moon
, Hyun Joo Shim
, Eun Jung Kim
, Soon Hoe Kim
, Joong In Lim
, Chun Ho Lee^*

^*Corresponding author for this work

Department of Pharmacy

Yuhan Research Institute
Dong-A Research Institute

Research output: Contribution to journal › Journal article › peer-review

9 Scopus citations

Abstract

Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC₅₀ of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.

Original language	English
Pages (from-to)	4993-4996
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2008.08.020
State	Published - 2008.09.15

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

PPARα/γ dual agonists
PPARs
Tetrahydropyridine
Type 2 diabetes

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10.1016/j.bmcl.2008.08.020

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Kim, E., Park, C. S., Han, T., Bae, M. H., Chong, W., Lee, C. H., Shin, Y. A., Ahn, B. N., Kim, M. K., Shin, C. Y., Son, M. H., Kim, J. K., Moon, H. S., Shim, H. J., Kim, E. J., Kim, S. H., Lim, J. I., & Lee, C. H. (2008). Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists. Bioorganic and Medicinal Chemistry Letters, 18(18), 4993-4996. https://doi.org/10.1016/j.bmcl.2008.08.020

@article{b529f51cca0343b1a0aa4ecd4ba4b758,

title = "Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists",

abstract = "Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.",

keywords = "PPARα/γ dual agonists, PPARs, Tetrahydropyridine, Type 2 diabetes",

author = "Eunkyung Kim and Park, \{Chan Sun\} and Taedong Han and Bae, \{Myung Ho\} and Wonee Chong and Lee, \{Choong Hyun\} and Shin, \{Young Ah\} and Ahn, \{Byung Nak\} and Kim, \{Mi Kyung\} and Shin, \{Chang Yell\} and Son, \{Moon Ho\} and Kim, \{Jin Kwan\} and Moon, \{Ho Sang\} and Shim, \{Hyun Joo\} and Kim, \{Eun Jung\} and Kim, \{Soon Hoe\} and Lim, \{Joong In\} and Lee, \{Chun Ho\}",

year = "2008",

month = sep,

day = "15",

doi = "10.1016/j.bmcl.2008.08.020",

language = "English",

volume = "18",

pages = "4993--4996",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

number = "18",

}

Kim, E, Park, CS, Han, T, Bae, MH, Chong, W, Lee, CH, Shin, YA, Ahn, BN, Kim, MK, Shin, CY, Son, MH, Kim, JK, Moon, HS, Shim, HJ, Kim, EJ, Kim, SH, Lim, JI & Lee, CH 2008, 'Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 18, pp. 4993-4996. https://doi.org/10.1016/j.bmcl.2008.08.020

TY - JOUR

T1 - Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists

AU - Kim, Eunkyung

AU - Park, Chan Sun

AU - Han, Taedong

AU - Bae, Myung Ho

AU - Chong, Wonee

AU - Lee, Choong Hyun

AU - Shin, Young Ah

AU - Ahn, Byung Nak

AU - Kim, Mi Kyung

AU - Shin, Chang Yell

AU - Son, Moon Ho

AU - Kim, Jin Kwan

AU - Moon, Ho Sang

AU - Shim, Hyun Joo

AU - Kim, Eun Jung

AU - Kim, Soon Hoe

AU - Lim, Joong In

AU - Lee, Chun Ho

PY - 2008/9/15

Y1 - 2008/9/15

N2 - Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.

AB - Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.

KW - PPARα/γ dual agonists

KW - PPARs

KW - Tetrahydropyridine

KW - Type 2 diabetes

UR - https://www.scopus.com/pages/publications/51349144381

U2 - 10.1016/j.bmcl.2008.08.020

DO - 10.1016/j.bmcl.2008.08.020

M3 - Journal article

C2 - 18771917

AN - SCOPUS:51349144381

SN - 0960-894X

VL - 18

SP - 4993

EP - 4996

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 18

ER -

Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists

Abstract

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Keywords

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