Synthesis and analgesic-antiinflammatory activity of some 4- and 5-substituted heteroarylsalicylic acids.

Autor: Jones H, Fordice MW, Greenwald RB, Hannah J, Jacobs A, Ruyle WV, Walford GL, Shen TY
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1978 Nov; Vol. 21 (11), pp. 1100-4.
DOI: 10.1021/jm00209a002
Abstrakt: 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.
Databáze: MEDLINE