S. Laneri et al., RESEARCH ON HETEROCYCLIC-COMPOUNDS - PART-XXXIX - 2-METHYLIMIDAZO[1,2-A]PYRIMIDINE-3-CARBOXYLIC DERIVATIVES - SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY, European journal of medicinal chemistry, 33(3), 1998, pp. 163-170
The synthesis of a group of 2-methylimidazo[1,2-a]pyrimidine-3-carboxy
lic esters, acids and amides is described. The structures of new compo
unds are supported by H-1 and C-13 NMR spectre. These compounds were t
ested in vivo for their antiinflammatory, analgesic. and ulcerogenic a
ctivity. Eight new compounds out of fifteen showed remarkable dose-dep
endent antiinflammatory action in the carrageenan rat paw edema (1/2-1
/3 x indomethacin) but weak analgesic activity in the acetic acid writ
hing test together with negligible ulcerogenic action. The new compoun
ds were found to be lacking in inhibitory activity on cyclooxygenase i
n vitro. (C) Elsevier, Paris.