Structure-activity relationships in a series of anti-inflammatory N-arylanthranilic acids

A large series of N-arylanthranilic acids has been prepared. Many of these compounds show high anti-inflammatory activity as measured by the anti-UV-erythema test. From this series have come the clinically useful non-steroidal anti-inflammatory agents, flufenamic acid (Arlef), mefenamic acid (Ponste...

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Published inArzneimittel-Forschung Vol. 33; no. 4A; p. 621
Main Authors Kaltenbronn, J S, Scherrer, R A, Short, F W, Jones, E M, Beatty, H R, Saka, M M, Winder, C V, Wax, J, Williamson, W R
Format Journal Article
LanguageEnglish
Published Germany 1983
Subjects
Animals
Anti-Inflammatory Agents - chemical synthesis
Chemical Phenomena
Chemistry
Erythema - drug therapy
Guinea Pigs
ortho-Aminobenzoates - chemical synthesis
ortho-Aminobenzoates - pharmacology
Structure-Activity Relationship
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Summary:A large series of N-arylanthranilic acids has been prepared. Many of these compounds show high anti-inflammatory activity as measured by the anti-UV-erythema test. From this series have come the clinically useful non-steroidal anti-inflammatory agents, flufenamic acid (Arlef), mefenamic acid (Ponstel), and the latest and most potent agent, N-(2,6-dichloro-m-tolyl)anthranilic acid (meclofenamic acid, Meclomen = the sodium salt). The structure-activity relationships of this series is discussed and a graphical representation is presented which allows the prediction of activity of new agents.
ISSN:0004-4172