Hussien A. Karim Ayad M. R. Raauf Karima F. Ali


Objective To synthesize and initial pharmacological assessment of new analogues of nabumetone by incorporating of pyrimidine heterocyclic ring systems into the nabumetone moiety to increase the activity toward COX enzymes. Examination of their in vivo results by using egg white to induce acute inflammation. Methods A series of pyrimidines bearing nabumetone moiety have been designed, synthesized, and evaluated as a potential COX- inhibitors. These new compounds were evaluated for their in vivo anti-inflammatory activity. Results All tested compounds have good results in acute anti-inflammatory in vivo tests better than nabumetone. Conclusion The synthesis of the designed compounds has been successfully achieved, the anti-inflammatory assessment of the final products indicates that the incorporation of pyrimidine pharmacophore into nabumetone improved its anti- inflammatory action, the Preliminary study of anti-inflammatory activity showed that compound (2a-2e especially 2c and 2d) have significantly more anti-inflammatory outcome than nabumetone.

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nabumetone, pyrimidine, chalcone, anti-inflammatory activity

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