Synthesis and evaluation of the analgesic and antiinflammatory activities of N-substituted salicylamides.
Some N-heterocyclic salicylamide derivatives were prepared by fusion of phenyl salicylate and heterocyclic amines, whereas other ones were synthesized by ring closure using N-salicyloyl-N'-anthranylhydrazine as starting material. All the compounds were tested for their analgesic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effects, in order to ascertain if the N-substitution would offer any advantages. Some derivatives were more effective than salicylamide and ulcerogenic activity was variably lowered.
Daidone
G
G
Dipartimento di Chimica, Facoltà di Farmacia, Università di Palermo, Italy.
Raffa
D
D
Plescia
S
S
Matera
M
M
Caruso
A
A
Leone
V
V
Amico-Roxas
M
M
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000633:toxicity; D001522:Behavior, Animal / Q000187:drug effects; D002351:Carrageenan; D055598:Chemical Phenomena; D002621:Chemistry; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005122:Exudates and Transudates / Q000187:drug effects; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D011930:Reaction Time / Q000187:drug effects; D012457:Salicylamides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D013276:Stomach Ulcer / Q000139:chemically induced
D000894:Anti-Inflammatory Agents, Non-Steroidal; D012457:Salicylamides; D002351:Carrageenan