Synthesis of new pyrimidine derivatives with evaluation of their anti-inflammatory and analgesic activities.

摘要: 5-Formyl-6-aminopyrimidine-2,4-(1H, 3H)-dione (2) has been previously prepared fromcompound 1. Cyclocondensation reaction of compound 2 with cyanoacetamide gave substituted pyridopyrimidine 3. Also, was condensed p-amino acetophenone and hydrazine derivatives to give 5-([(4-acetylphenyl)imino]methyl)-6-aminopyrimidine (4) 5-substituted carboaldehyde-6-amino pyrimidine (5a-d), respectively. Moreover, cyclocondensation thiosemcarbazide semicarbazide hydrochloride 5-(5-thioxo or oxo-triazol-3-yl)-6-amino (6) (7), thiourea ethyl acetoacetate led the formation bipyrimidine-5-carboxylate 8. reacted acetoacetic acid hydrazide 2-cyanoacetohydrazide 5-(acetylpyrazol-6-aminopyrimidine 9 3-(6-aminopyrimidine-5-yl) pyrazole-4-carboxamide 10, Furthermore, 1 diazotized afford diazonium salt 11. Its coupling acetoacetate, cyanoacetate, acetylacetone, malononitrile, cyanoacetamide, diethylmalonate, in sodium acetate buffered solution afforded hydrazonopyrimidines: ethylhydrazono-3-oxobutanoate 12, ethylhydrazono-3-oxopropanoate 13, pentane-2,3,4-trione hydrazone 14, cyanohydrazonoacetamide 15, diazenyl malonamide 16 diethylhydrazonomalonate 17, pyrazolediazenylpyrimidine 18a,b, 19a,b, 20, 21a-c, 22 were synthesized by cyclization hydrazonopyrimidines 14 The analgesic anti-inflammatory activities some compounds evaluated. Compounds C18a, C20, C21b C22 showed most significant effects among moieties. All tested compounds, nonetheless, C18b effect carrageenan induced paw edema model.