5-substituted 4-isoxazoleacetic acids with analgesic activity.
The synthesis of some 5-substituted 4-isoxazoleacetic acids starting from 5-substituted 4-isoxazolemethanols via their conversion to 4-(bromomethyl)isoxazoles, 4-isoxazoleacetonitriles and acid hydrolysis of the latter is described. 5-Ethyl- and 5-propyl-4-isoxazoleacetic acids showed in the writhing test an analgesic activity comparable to that of aspirin.
Fossa
P
P
Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.
Menozzi
G
G
Schenone
P
P
Mattioli
F
F
D000085:Acetates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D013055:Spectrophotometry, Infrared
D000085:Acetates; D000700:Analgesics; D007555:Isoxazoles; D002351:Carrageenan