Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry


Microwave assisted synthesis of some 5-substituted imidazolone analogs as a new class of non purine xanthine oxidase inhibitors .

Author(s): Bhawna Chopra 1,2 , Ashwani Kumar Dhingra 1,2 , Ram Parkash Kapoor 1 and Deo Nandan Parsad 3

A series of 5-substituted imidazolone 1-22 analogs were synthesized by condensation of different substituted oxazolones with various aromatic amines under solvent free conditions in a microwave reacto r. All the synthesised compounds were evaluated for in vitro xanthine oxid ase inhibitory activity for the first time. Xanthin e oxidase is a complex molybdoflavoprotein that catalyses the hydr oxylation of xanthine to uric acid. Among the synth esised compounds 7 , 11 , 13 , 15 and 19 were found to be most active inhibitors with an IC 50 ranging from 6 to 20.28 μM. Compound 7 emerged as the most potent xanthine oxidase inhibit or (IC 50 = 6 μ M) in comparison to allopurinol (IC 50 = 11.10 μ M). The structures of all the newly synthesized compoun ds were elucidated by using IR, 1 H-NMR