Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARγ activators

Bioorganic & Medicinal Chemistry Letters
2007.0

Abstract

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.

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