Synthesis of 1-methyl-4-(N-aroyl)-piperidinamides with anti-inflammatory and analgesic activities.
Two series of 1-methyl-4-(N-aroyl)-piperidinamides were synthesized and evaluated for their anti-inflammatory and analgesic properties, as well as for their gastrointestinal irritation liability. A non-aromatic derivative, 1-methyl-4-(N-cyclohexanoyl)-piperidinamide, was synthesized and evaluated in order to obtain a more exhaustive knowledge of the structure-activity relationship.
Pau
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Istituto di Analitica Farmaceutica, Facoltà di Farmacia, Università di Sassari, Italy.
Boatto
G
G
Cerri
R
R
Palagiano
F
F
Filippelli
W
W
Falcone
G
G
Lampa
E
E
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D004487:Edema / Q000188:drug therapy; D005260:Female; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000577:Amides; D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D010880:Piperidines