1227077-75-9Relevant academic research and scientific papers
Discovery of a novel selective PPARγ modulator from (-)-Cercosporamide derivatives
Furukawa, Akihiro,Arita, Tsuyoshi,Satoh, Susumu,Wakabayashi, Kenji,Hayashi, Shinko,Matsui, Yumi,Araki, Kazushi,Kuroha, Masanori,Ohsumi, Jun
scheme or table, p. 2095 - 2098 (2010/08/22)
In an investigation of (-)-Cercosporamide derivatives with a plasma glucose-lowering effect, we found that N-benzylcarboxamide derivative 4 was a partial agonist of PPARγ. A SAR study of the substituents on carboxamide nitrogen afforded the N-(1-naphthyl)methylcarboxamide derivative 23 as the most potent selective PPARγ modulator. An X-ray crystallography study revealed that compound 23 bounded to the PPARγ ligand binding domain in a unique way without any interaction with helix12. Compound 23 displayed a potent plasma glucose-lowering effect in db/db mice without the undesirable increase in body fluid and heart weight that is typically observed when PPARγ full agonists are administrated.
