Substituted (2-phenoxyphenyl)acetic acids with antiinflammatory activity. 1

The synthesis and antiinflammatory activity of a series of substituted (2-phenoxyphenyl)acetic acids are described. Initial screening in the adjuvant arthritis test showed that halogen substitution in the phenoxy ring enhanced activity considerably. Ulcerogenic potential, as measured by the minimum...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1983-10, Vol.26 (10), p.1353-1360
Main Authors: Atkinson, David C, Godfrey, Keith E, Meek, Bernard, Saville, John F, Stillings, Michael R
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - therapeutic use
Arthritis, Experimental - drug therapy
Drug Evaluation, Preclinical
Indicators and Reagents
Phenylacetates - therapeutic use
Rats
Spectrophotometry, Infrared
Structure-Activity Relationship
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Summary:The synthesis and antiinflammatory activity of a series of substituted (2-phenoxyphenyl)acetic acids are described. Initial screening in the adjuvant arthritis test showed that halogen substitution in the phenoxy ring enhanced activity considerably. Ulcerogenic potential, as measured by the minimum ulcerogenic dose (MUD), was low in almost all the acids tested. [2-(2,4-Dichlorophenoxy)phenyl]acetic acid possessed the most favorable combination of potency with low toxicity, including ulcerogenicity, and this compound is now in therapeutic use.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00364a004