Research on heterocyclic compounds. XXX. Synthesis and pharmacological activity of 2-methylimidazo[1,2-b]pyridazine-3-carboxylic acids.
A group of ethyl 2-methylimidazo[1,2-b]pyridazine-3-carboxylates were prepared by reaction in anhydrous ethanol of some substituted 3-amino-pyridazines with ethyl 2-chloroacetoacetate. The corresponding carboxylic acids were obtained via alkaline or acid hydrolysis and then tested both in vivo to evaluate their antiinflammatory, analgesic and ulcerogenic actions and in vitro for their ability to inhibit the prostaglandin biosynthesis. The pharmacological results are discussed in terms of both structure-activity relationships and mechanism of action.
Abignente
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E
Dipartimento di Chimica Farmaceutica e Tossicologica Facoltà di Farmacia, Università di Napoli Federico II, Italy.
Arena
F
F
Luraschi
E
E
Saturnino
C
C
Rossi
F
F
Berrino
L
L
Cenicola
M L
ML
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D004487:Edema / Q000139:chemically induced / Q000473:pathology; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008315:Malondialdehyde / Q000097:blood; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000517:prevention & control; D011247:Pregnancy; D011448:Prostaglandin Antagonists; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013056:Spectrophotometry, Ultraviolet; D013276:Stomach Ulcer / Q000139:chemically induced; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D011448:Prostaglandin Antagonists; D011724:Pyridazines; C077427:2-methylimidazo(1,2-b)pyridazine-3-carboxylic acid; D008315:Malondialdehyde