Indenone Derivatives: A Novel Template for Peroxisome Proliferator-Activated Receptor γ (PPARγ) Agonists

Agonists of peroxisome proliferator-activated receptor γ (PPAR γ) are of interest as a treatment for diabetes, which prompted the identification of a new class of non-TZD PPAR γ agonist. Moreover, compound 14c has displayed the most active agonistic activity with an EC50 value of 50 nM, in addition...

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Veröffentlicht in:	Journal of medicinal chemistry 2006-07, Vol.49 (15), p.4781-4784
Hauptverfasser:	Ahn, Jin Hee, Shin, Mi Sik, Jung, Sun Ho, Kang, Seung Kyu, Kim, Kwang Rok, Rhee, Sang Dal, Jung, Won Hoon, Yang, Sung Don, Kim, Seung Jun, Woo, Joo Rang, Lee, Jeong Hyung, Cheon, Hyae Gyeong, Kim, Sung Soo
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Crystallography, X-Ray General and cellular metabolism. Vitamins Humans Indenes - chemical synthesis Indenes - chemistry Indenes - pharmacology Ligands Medical sciences Mice Models, Molecular Molecular Structure NIH 3T3 Cells Pharmacology. Drug treatments PPAR gamma - agonists PPAR gamma - chemistry
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Zusammenfassung:	Agonists of peroxisome proliferator-activated receptor γ (PPAR γ) are of interest as a treatment for diabetes, which prompted the identification of a new class of non-TZD PPAR γ agonist. Moreover, compound 14c has displayed the most active agonistic activity with an EC50 value of 50 nM, in addition to exhibiting a new binding mode in the X-ray cocrystal structure.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm060389m