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

…, MW Fordice, RB Greenwald, J Hannah…

Index: Jones; Fordice; Greenwald; Hannah; Jacobs; Ruyle; Walford; Shen Journal of Medicinal Chemistry, 1978 , vol. 21, # 11 p. 1100 - 1104

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Citation Number: 25

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. ...