Details

Autor(en) / Beteiligte

• Devasthale, Pratik V
• Chen, Sean
• Jeon, Yoon
• Qu, Fucheng
• Shao, Chunning
• Wang, Wei
• Zhang, Hao
• Cap, Michael
• Farrelly, Dennis
• Golla, Rajasree
• Grover, Gary
• Harrity, Thomas
• Ma, Zhengping
• Moore, Lisa
• Ren, Jimmy
• Seethala, Ramakrishna
• Cheng, Lin
• Sleph, Paul
• Sun, Wei
• Tieman, Aaron
• Wetterau, John R
• Doweyko, Arthur
• Chandrasena, Gamini
• Chang, Shu Y
• Humphreys, W. Griffith
• Sasseville, Vito G
• Biller, Scott A
• Ryono, Denis E
• Selan, Fred
• Hariharan, Narayanan
• Cheng, Peter T. W

Titel

Design and Synthesis of N-[(4-Methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a Novel Peroxisome Proliferator-Activated Receptor α/γ Dual Agonist with Efficacious Glucose and Lipid-Lowering Activities

Ist Teil von

• Journal of medicinal chemistry, 2005-03, Vol.48 (6), p.2248-2250

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

2005

Quelle

MEDLINE

Beschreibungen/Notizen

• Muraglitazar/BMS-298585 (2) has been identified as a non-thiazolidinedione PPAR α/γ dual agonist that shows potent activity in vitro at human PPARα (EC50 = 320 nM) and PPARγ (EC50 = 110 nM). Compound 2 shows excellent efficacy for lowering glucose, insulin, triglycerides, and free fatty acids in genetically obese, severely diabetic db/db mice and has a favorable ADME profile. Compound 2 is currently in clinical development for the treatment of type 2 diabetes and dyslipidemia.