[Derivatives of 2-phenothiazin-2'-yl-cinchoninic acid with analgesic and anti-inflammatory activity].
In order to investigate the effects of the overlapping of cinchophene and phenothiazine structures, connected with antiinflammatory and analgesic activities, several derivatives of 2-phenothiazin-2'-yl-cinchoninic acid were prepared through the condensation of isatin or 5-substituted isatins with 2-acetylphenothiazine or its 10-ter-aminoalkyl derivatives. Most of these compounds exhibit analgesic activity, but only a few, of those so far tested, show antiinflammatory activity. Compound (G) with R' = H, R" = C2H5 and R"' = dimethylaminoethyl shows analgesic activity corresponding to 88% of that of phenylbutazone. Moreover some compounds show signs of sympatholytic and vasodilatatory activities and also bactericidal and amebicidal properties in vitro, while some others demonstrate a modest neuroplegic activity.
D000661:Amphetamine / Q000037:antagonists & inhibitors; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis*; D000927:Anticonvulsants; D001463:Barbiturates / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D004347:Drug Interactions; D006168:Guinea Pigs; D066298:In Vitro Techniques; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D010640:Phenothiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D012110:Reserpine / Q000037:antagonists & inhibitors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D001463:Barbiturates; D010640:Phenothiazines; D011804:Quinolines; D012110:Reserpine; D000661:Amphetamine
Derivati dell'acido 2-fenotiazin-2'-il-cinconinico ad attività analgesico-antiinfiammatoria.