Substituents at the naphthalene C3 position of (−)-Cercosporamide derivatives significantly affect the maximal efficacy as PPARγ partial agonists

Peroxisome proliferator-activated receptor gamma (PPARγ) is a potential drug target for treating type 2 diabetes. The selective PPARγ modulators (SPPARMs), which partially activate the PPARγ transcriptional activity, are considered to improve the plasma glucose level with attenuated PPARγ related ad...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-02, Vol.22 (3), p.1348-1351
Hauptverfasser:	Furukawa, Akihiro, Arita, Tsuyoshi, Fukuzaki, Takehiro, Satoh, Susumu, Mori, Makoto, Honda, Takeshi, Matsui, Yumi, Wakabayashi, Kenji, Hayashi, Shinko, Araki, Kazushi, Ohsumi, Jun
Format:	Artikel
Sprache:	eng
Schlagworte:	(−)-Cercosporamide adverse effects agonists Benzofurans - chemical synthesis Benzofurans - chemistry Benzofurans - pharmacology Biological and medical sciences blood glucose Crystallography, X-Ray Diabetes Diabetes mellitus Drugs Gene Expression Regulation - drug effects Glucose Humans Hypoglycemic Agents - chemical synthesis Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Inhibitory Concentration 50 Medical sciences Models, Molecular Molecular Structure Naphthalene Naphthalenes - chemistry noninsulin-dependent diabetes mellitus Peroxisome proliferator-activated receptors Pharmacology. Drug treatments PPAR gamma - agonists PPARγ modulator Side effects SPPARM SPPARγM Transcription transcription (genetics)
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