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 alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
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Devasthale PV, Chen S, Jeon Y, Qu F, Shao C, Wang W, Zhang H, Cap M, Farrelly D, Golla R, Grover G, Harrity T, Ma Z, Moore L, Ren J, Seethala R, Cheng L, Sleph P, Sun W, Tieman A, Wetterau JR, Doweyko A, Chandrasena G, Chang SY, Humphreys WG, Sasseville VG, Biller SA, Ryono DE, Selan F, Hariharan N, Cheng PT
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 alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
J Med Chem. 2005 Mar 24;48(6):2248-50.
- PubMed ID
- 15771468 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha IC 50 (nM) >100000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) >32000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma IC 50 (nM) 250 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 140 N/A N/A Details