Structure Activity Relationship Among 6-Substituted-2-Naphthylacetic Acids: A New Series of Nonsteroidal Anti-inflammatory Agents

J. H. Fried Institutes of Organic Chemistry and Biological Sciences, Syntex Research, Stanford Industrial Park, Palo Alto, California, USA

I. T. Harrison Institutes of Organic Chemistry and Biological Sciences, Syntex Research, Stanford Industrial Park, Palo Alto, California, USA

B. Lewis Institutes of Organic Chemistry and Biological Sciences, Syntex Research, Stanford Industrial Park, Palo Alto, California, USA

J. Riegl Institutes of Organic Chemistry and Biological Sciences, Syntex Research, Stanford Industrial Park, Palo Alto, California, USA

W. Rooks Institutes of Organic Chemistry and Biological Sciences, Syntex Research, Stanford Industrial Park, Palo Alto, California, USA

A. Tomolonis Institutes of Organic Chemistry and Biological Sciences, Syntex Research, Stanford Industrial Park, Palo Alto, California, USA

Abstract

Chemical modification of 2-naphthylacetic acid has led to (+)-2-(6-methoxy-2-naphthyl)-propionic acid, naproxen. Maximal biological activity in the naph-thylpropionic acid series is associated with the S absoiuti configuration. In experimental animals naproxen shows anti-inflammatory, analgetic and antipyretic activity o: llxphenylbutazone, and 7 and 22xacetylsalicylic acid re spectively. It is noteworthy that highly active compound! were obtained without resorting to nitrogenous substitu cnts.

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Structure Activity Relationship Among 6-Substituted-2-Naphthylacetic Acids: A New Series of Nonsteroidal Anti-inflammatory Agents

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Structure Activity Relationship Among 6-Substituted-2-Naphthylacetic Acids: A New Series of Nonsteroidal Anti-inflammatory Agents

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