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Original Article

ECB. 2016; 5(8): 348-353


SYNTHESIS AND ANTI-INFLAMMATORY ACTIVITY OF SOME NEW PYRAZOLO[3,4-d] PYRIMIDINES

Adel M. Kamal El-Dean, Shawkat A. Abdel-Mohsen,Yasser A. Elossaily, Istabrak I .Hussein.




Abstract

5-Amino-3-methyl-1-phenyl-1H-pyrazole-4-carbonitrile (5) was reacted with chloroacetyl chloride under fusion condition to afford two
compounds, which identified as 6-chloromethylpyrazolo[3,4-d]pyrimdine (3) and 4-amino-5-chloropyrazolo[3,4-b]pyridine (7) ln different
ratios. Treatment of compound (3) with aromatic amines, gave the arylaminomethyl derivatives (8a-c). Compound (3) was reacted with
sodium azide, phosphorous oxychloride, sulphanilamide to give new derivatives (9, 10, and 14). The 4-chloro derivative (11) underwent
nucleophilic substitution using some reagent such as P2S5, sodium azide and hydrazine hydrate to furnish novel pyrazolo[3,4-d]pyrimidines
(12, 13, 15, 16, 17). All synthesized compounds were characterized using elemental analysis and spectral techniques. The antiinflammatory activity of all the newly synthesized compounds was evaluated using the carrageenan induced paw oedema test in
rats using indomethacin as the reference drug.

Key words: : Pyrazolo[3,4-d]pyrimidinone, 6-aryaminomethyl derivatives, sulfa drug, tetrazole, anti-inflammatory activity.






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