Anti-inflammatory and analgesic amides: new developments.
A series of substituted N-cycloalkyl benzamides, cinnamamides, and indole-3-carboxamides were synthesized and evaluated for their analgesic, antiinflammatory activities as well as for their gastrointestinal irritation liability. Indomethacin was used as reference drug in both tests. Compounds 1k, 1b, 1h, 1j, and 1g were the most active in the antiinflammatory paw edema inhibition test, with a sharply dose-dependent effect. In terms of the analgesic activity (acetic acid writhing test), the most active compound was 5a followed by 3a, but many other compounds were found to have a non-negligible potency. Even in this case, the effect was dose dependent.
Palomba
M
M
Dipartimento Farmaco Chimico Tossicologico, Facoltà di Farmacia, Università di Sassari, Italy.
Pau
A
A
Boatto
G
G
Asproni
B
B
Auzzas
L
L
Cerri
R
R
Arenare
L
L
Filippelli
W
W
Falcone
G
G
Motola
G
G
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D008297:Male; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced; D013329:Structure-Activity Relationship
D000577:Amides; D000894:Anti-Inflammatory Agents, Non-Steroidal