title: Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents.
abstract: In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing α-alkoxy-phenylpropanoic acid derivatives are designed as highly potent PPARα/γ dual agonists. These compounds were found to be efficacious at picomolar concentrations. Lead compound 18d has emerged as very potent PPARα/γ dual agonist demonstrating potent antidiabetic and lipid lowering activity at a very low dose and did not exhibit any significant signs of toxicity in rodents.
authors: Zydus Research Centre, Sarkhej-Bavla N.H 8A Moraiya, Ahmedabad 382210, India. preetiraval@zyduscadila.com
authors: Preeti
authors: P
authors: Raval
authors: Mukul
authors: M
authors: Jain
authors: Amitgiri
authors: A
authors: Goswami
authors: Sujay
authors: S
authors: Basu
authors: Archana
authors: A
authors: Gite
authors: Atul
authors: A
authors: Godha
authors: Harikishore
authors: H
authors: Pingali
authors: Saurin
authors: S
authors: Raval
authors: Suresh
authors: S
authors: Giri
authors: Dinesh
authors: D
authors: Suthar
authors: Maanan
authors: M
authors: Shah
authors: Pankaj
authors: P
authors: Patel
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D010080:Oxazoles / Q000737:chemistry; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D000077154:Rosiglitazone; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013876:Thiophenes / Q000737:chemistry
chemical_list: D007004:Hypoglycemic Agents; D010080:Oxazoles; D047493:PPAR alpha; D047495:PPAR gamma; D010666:Phenylpropionates; D045162:Thiazolidinediones; D013876:Thiophenes; D000077154:Rosiglitazone