Research on heterocyclic compounds — Part XXXIX. 2-Methylimidazo[1,2-a]pyrimidine-3-carboxylic derivatives: Synthesis and antiinflammatory activity
摘要:
The synthesis of a group of 2-methylimidazo[1,2-a]pyrimidine-3-carboxylic esters, acids and amides is described. The structures of new compounds are supported by H-1 and C-13 NMR spectre. These compounds were tested in vivo for their antiinflammatory, analgesic. and ulcerogenic activity. Eight new compounds out of fifteen showed remarkable dose-dependent antiinflammatory action in the carrageenan rat paw edema (1/2-1/3 x indomethacin) but weak analgesic activity in the acetic acid writhing test together with negligible ulcerogenic action. The new compounds were found to be lacking in inhibitory activity on cyclooxygenase in vitro. (C) Elsevier, Paris.
The synthesis of a group of 2-methylimidazo[1,2-a]pyrimidine-3-carboxylic esters, acids and amides is described. The structures of new compounds are supported by H-1 and C-13 NMR spectre. These compounds were tested in vivo for their antiinflammatory, analgesic. and ulcerogenic activity. Eight new compounds out of fifteen showed remarkable dose-dependent antiinflammatory action in the carrageenan rat paw edema (1/2-1/3 x indomethacin) but weak analgesic activity in the acetic acid writhing test together with negligible ulcerogenic action. The new compounds were found to be lacking in inhibitory activity on cyclooxygenase in vitro. (C) Elsevier, Paris.
Abignente; Arena; Luraschi, Farmaco, Edizione Scientifica, 1984, vol. 39, # 5, p. 379 - 388