5-substituted 4-isoxazolecarboxamides with platelet antiaggregating and other activities.
The synthesis of a series of 5-substituted 4-isoxazolecarboxamides by reaction of eight 5-substituted 4-isoxazolecarbonyl chlorides with pyrrolidine, piperidine, morpholine and 4-trifluoromethylaniline is described. Some of these amides showed platelet antiaggregating activity in vitro slightly inferior to that of acetylsalicylic acid, as well weak antiinflammatory, analgesic and antipyretic activities in rats and mice.
Fossa
P
P
Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.
Menozzi
G
G
Schenone
P
P
Filippelli
W
W
Russo
S
S
Lucarelli
C
C
Marmo
E
E
D000814:Aniline Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D009025:Morpholines / Q000138:chemical synthesis / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D013055:Spectrophotometry, Infrared
D000814:Aniline Compounds; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007555:Isoxazoles; D009025:Morpholines; D010880:Piperidines; D010975:Platelet Aggregation Inhibitors; D011759:Pyrrolidines