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

E Kim, CS Park, T Han, MH Bae, W Chong…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 4993 - 4996

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Citation Number: 8

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.