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

Journal of Medicinal Chemistry
2005.0

Abstract

Muraglitazar/BMS-298585 (2) has been identified as a non-thiazolidinedione PPAR alpha/gamma dual agonist that shows potent activity in vitro at human PPARalpha (EC(50) = 320 nM) and PPARgamma(EC(50) = 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.

Knowledge Graph

Similar Paper

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
Journal of Medicinal Chemistry 2005.0
Discovery of a Novel Series of Peroxisome Proliferator-Activated Receptor α/γ Dual Agonists for the Treatment of Type 2 Diabetes and Dyslipidemia
Journal of Medicinal Chemistry 2005.0
(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl)propanoic acid compounds: Synthesis and biological evaluation of dual PPARα/γ agonists
Bioorganic & Medicinal Chemistry Letters 2010.0
Design and Synthesis of Dual Peroxisome Proliferator-Activated Receptors γ and δ Agonists as Novel Euglycemic Agents with a Reduced Weight Gain Profile
Journal of Medicinal Chemistry 2006.0
Design, Synthesis, and Biological Evaluation of Novel Constrained meta-Substituted Phenyl Propanoic Acids as Peroxisome Proliferator-Activated Receptor α and γ Dual Agonists
Journal of Medicinal Chemistry 2008.0
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1)
Bioorganic & Medicinal Chemistry Letters 2012.0
Revisiting glitazars: Thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents
Bioorganic & Medicinal Chemistry Letters 2011.0
Design and synthesis of a novel class of dual PPARγ/δ agonists
Bioorganic & Medicinal Chemistry Letters 2007.0
Design and synthesis of novel and potent amide linked PPARγ/δ dual agonists
Bioorganic & Medicinal Chemistry Letters 2007.0
Design and Synthesis of 2-Methyl-2-{4-[2-(5-methyl-2-aryloxazol- 4-yl)ethoxy]phenoxy}propionic Acids:  A New Class of Dual PPARα/γ Agonists
Journal of Medicinal Chemistry 2001.0