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Synthesis and Biological activity of new 5-Methyl-3-Oxo-N2 [5’- Carbonyl-(4’-Aryl-6’methyl)-1’,2’,3’,4’–Tetrahydropyrimidine-2’- One]Pyrazolidines


Radhika C , Venkatesham A , Anantha Krishna Chaitanya D

Abstract

A number of new pyrimidine fused pyrazolidine derivatives have been synthesized starting from the preparation of tetrahydro pyrimidine derivatives which utilised the involvement of biginelli reaction.Finally, clinical candidates were obtained by the reaction of ary hydrazine with ethyl acetoacetate,P-toluene sulfonic acid and ethanol . The structure of compounds was confirmed by IR, and (1) H-NMR data. The synthesized compounds were evaluated for their antiinflammatory activity against Formalin-induced pedal inflammation in albino rats at a dose of 50.75 and 100mg/kg. The most active compound of this series is 5- methyl-3-oxo-N2[5’-carbonyl-(4-(4-methoxy phenyl)-6’-methyl)-1’,2’,3’,4’- tetrahydro pyrimidine-2’-one] pyrazolidine 4a) was found to be most potent, which has shown higher percent of inhibition of oedema than than the standard drug Diclofenac sodium.



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