Synthesis and analgesic-antiinflammatory activity of some 4- and 5-substituted heteroarylsalicylic acids.
We have made a series of 4- and 5-aryl- and 4- and 5-heteroarylsalicylic acid derivatives with the objective of reducing gastric irritation and increasing potency. Here we describe a series of 4- and 5-heterocyclic salicylic acids and their antiinflammatory-analgesic potencies measured in comparison to aspirin. An improvement of the therapeutic index over aspirin of 100 was achieved; however, the heterocyclic salicylic acids lacked antipyretic activity. Some physicochemical parameters which may bear on the antiinflammatory activity of these compounds are discussed.
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004285:Dogs; D004487:Edema / Q000503:physiopathology; D006471:Gastrointestinal Hemorrhage / Q000139:chemically induced; D051381:Rats; D012459:Salicylates / Q000138:chemical synthesis* / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D012459:Salicylates