Antagonists of slow reacting substance of anaphylaxis. Synthesis of a series of chromone-2-carboxylic acids

A series of substituted chromone-2-carboxylic acids was synthesized and tested as antagonists of SRS-A induced contractions of isolated guinea pig ileum. This work led to the discovery of sodium 7-[3-(4-acetyl-3hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propyl-4H-1-benzopyran-2-carboxylate (...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1977-03, Vol.20 (3), p.371-379
Main Authors: Appleton, R. A, Bantick, J. R, Chamberlain, T. R, Hardern, D. N, Lee, T. B, Pratt, A. D
Format: Article
Language:English
Subjects:
Animals
Chromones - chemical synthesis
Chromones - pharmacology
Guinea Pigs
In Vitro Techniques
Methods
Muscle Contraction - drug effects
Muscle, Smooth - drug effects
SRS-A - antagonists & inhibitors
Structure-Activity Relationship
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Summary:A series of substituted chromone-2-carboxylic acids was synthesized and tested as antagonists of SRS-A induced contractions of isolated guinea pig ileum. This work led to the discovery of sodium 7-[3-(4-acetyl-3hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propyl-4H-1-benzopyran-2-carboxylate (FPL 55712) which is the first reported specific antagonist of SRS-A. Some structural requirements for biological activity within this series are discussed.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00213a012