Journal of Advanced Pharmacy Education & Research
 
 
Year : 2014   |  Volume : 4   |  Issue : 1   |  Page : 66-70  

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

Correspondence Address:Jawaharlal Nehru Technological University, Hyderabad-500085, Andhra Pradesh, India.

Source of Support: None, Conflict of Interest: None


DOI: 10.4103/2231-4040.197331

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.

Keywords: Biginelli Reaction, P-toluene sulfonic acid, Anti-inflammatory activity, Formalin, Diclofenac sodium

How to cite this article:
Radhika C*, Venkatesham A,

Introduction   Top

Materials and methods   Top

Results Discussion   Top

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