Synthesis, Analgesic and Ulcerogenic Activity of Novel Pyrimidine Derivative of Coumarin Moiety

A novel series of 3-(2-amino-6-pyrimidin-4-yl)-6-bromo-2H-chromen-2-one (5a-5j) were synthesized from 3-acetyl-6-bromo-2H-chromen-2-one (3). The structures of the synthesized compounds were elucidated by IR, H-NMR, C-NMR, and mass spectroscopic techniques. The synthesized compounds were screened for in-vivo analgesic activity at a dose of 20 mg/kg body weight. Among them, compounds 5a, 5b and 5e exhibited significant analgesic activity and compounds 5i and 5j exhibited highly significant activity comparable with standard drug Diclofenac sodium using Acetic acid induced writhing model. Compounds 5a, 5i and 5j were further evaluated for acute-ulcerogenesis activity. Among them, compound 5j was found to be most promising analgesic agent devoid of ulcerogenic effects. key words: Coumarin; Pyrimidines; Knoevenagel reaction; Claisen-schmidt condensation; Writhing Test; Analgesic activity; Ulcerogenic activity. received: September 9, 2010 accepted: October 7, 2010