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

Abstract

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.

Cite this paper

@article{Jones1978SynthesisAA, title={Synthesis and analgesic-antiinflammatory activity of some 4- and 5-substituted heteroarylsalicylic acids.}, author={Hayley M. Jones and M W Fordice and Richard B. Greenwald and Jessica A Hannah and An Jacobs and W. V. Ruyle and Geoffrey Walford and Tsung Ying Shen}, journal={Journal of medicinal chemistry}, year={1978}, volume={21 11}, pages={1100-4} }