Literature DB >> 18771917

Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.

Eunkyung Kim1, 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.   

Abstract

Aryl-tetrahydropyridine derivatives were prepared and their PPARalpha/gamma dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARalpha/gamma dual agonist with an EC(50) of 1.73 and 0.64 microM in hPPARalpha and gamma, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.

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Year:  2008        PMID: 18771917     DOI: 10.1016/j.bmcl.2008.08.020

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate.

Authors:  William Nguyen; Brittany L Howard; David P Jenkins; Heike Wulff; Philip E Thompson; David T Manallack
Journal:  Bioorg Med Chem Lett       Date:  2012-09-29       Impact factor: 2.823

2.  Effects of β-sitosterol derived from Artemisia capillaris on the activated human hepatic stellate cells and dimethylnitrosamine-induced mouse liver fibrosis.

Authors:  Ki-Suk Kim; Hea Jung Yang; Jae-Youl Lee; Yun-Cheol Na; Soo-Young Kwon; Young-Chul Kim; Jang-Hoon Lee; Hyeung-Jin Jang
Journal:  BMC Complement Altern Med       Date:  2014-09-27       Impact factor: 3.659

  2 in total

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