Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARgamma activators.
The design and synthesis of novel series of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid (pyrimidone) derivatives that are high affinity ligands for peroxisome proliferators activated receptor gamma have been reported as a potential substitute of 2,4-thiazolidinedione head group. The FlexX docking and radioligand binding affinity of some promising compounds of this series is comparable to that of thiazolidinedione based antidiabetic drugs currently in clinical use.
Kumar
Rakesh
R
Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India. rakvats@gmail.com
Mittal
Amit
A
Ramachandran
Uma
U
D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D047495:PPAR gamma / Q000819:agonists*; D011485:Protein Binding; D013329:Structure-Activity Relationship
D002264:Carboxylic Acids; D007004:Hypoglycemic Agents; D047495:PPAR gamma