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

The synthesis of the potent PPARα/γ dual agonist (S)-5b (EC 50 = 1.73/0.64 μM (α/γ)) is reported. 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 EC 50 of...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry Vol. 18; no. 18; pp. 4993 - 4996
Main Authors Kim, Eunkyung, Park, Chan Sun, Han, Taedong, Bae, Myung-Ho, Chong, Wonee, Lee, Choong Hyun, Shin, Young Ah, Ahn, Byung-Nak, Kim, Mi Kyung, Shin, Chang Yell, Son, Moon Ho, Kim, Jin Kwan, Moon, Ho Sang, Shim, Hyun Joo, Kim, Eun Jung, Kim, Soon Hoe, Lim, Joong In, Lee, Chun Ho
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 15.09.2008
Subjects
PPARs
PPARα/γ dual agonists
Tetrahydropyridine
Type 2 diabetes
Type 2 diabetes
PPARα/γ dual agonists
Tetrahydropyridine
PPARs
Online AccessGet full text

Cover

More Information
Summary:The synthesis of the potent PPARα/γ dual agonist (S)-5b (EC 50 = 1.73/0.64 μM (α/γ)) is reported. 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 EC 50 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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.08.020