F. Arena

Research on heterocyclic compounds, XLI. 2-Phenylimidazo[1,2-b]pyridazine-3-acetic derivatives: synthesis and anti-inflammatory activity

Abstract The synthesis of a group of 2-phenylimidazo[1,2-b]pyridazine-3-acetic esters and acids is described. The structures of the new compounds are supported by 1 H-NMR spectra. These compounds were tested in vivo for their anti-inflammatory, analgesic and ulcerogenic activity. All new compounds showed remarkable anti-inflammatory action in the carrageenan rat paw oedema (one third of that for indomethacin) but no significant analgesic activity in the acetic acid writhing test together with negligible ulcerogenic action, and were also found to be lacking inhibitory activity on cyclooxygenase in vitro.

Research on heterocyclic compounds — Part XXXIX. 2-Methylimidazo[1,2-a]pyrimidine-3-carboxylic derivatives: Synthesis and antiinflammatory activity

Abstract 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 1 H and 13 C NMR spectra. These compounds were tested in vivo for their antiinflammatory, analgesic and ulcerogenic activity. Eight new compounds out of fifteenshowed remarkable dose-dependent antiinflammatory action in the carrageenan rat paw edema (1/2–1/3 × 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.

2‐Phenylimidazo[1,2‐a]pyridine‐3‐carboxylic Acid Derivatives: Synthesis and Antiinflammatory Activity

A series of 2‐phenylimidazo[1,2‐a]pyridine‐3‐carboxylic esters, acids, and amides were synthesized and pharmacologically tested in order to evaluate their antiinflammatory and analgesic activity and their ulcerogenic action on the gastro‐intestinal tract. The most active member of this series of compounds was found to be 6‐methyl‐2‐phenylimidazo[1,2‐a]pyridine‐3‐carboxylic acid (5c).