Research on heterocyclic compounds. XXXVII. Synthesis and antiinflammatory activity of methyl-substituted imidazo[1,2-a]pyrazine derivatives

Article abstract of DOI:10.1016/S0223-5234(97)83971-2

A series of methyl-substituted imidazo[1,2-a]pyrazines 8 bearing a carboxylic acid group on the imidazole ring were synthesized. The structures of new compounds were confirmed by ¹H- and ¹³C-NMR spectral data; the correct assignment of carbon resonances was made by means of HETCOR and COLOC experiments. Antiinflammatory, analgesic and ulcerogenic activities in vivo were evaluated and compared with those of antiinflammatory imidazopyrazines (2 and 3) and indomethacin. The inhibitory action on cyclooxygenase activity was evaluated in vitro. Compounds 8 were found to be less potent than indomethacin in these assays. SARs are discussed.