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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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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
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cited_by cdi_FETCH-LOGICAL-a353t-844d6c1364a446428856f1d9c1210a7dac0349ba12380e1f534518cf5f6ac5ac3
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container_end_page 379
container_issue 3
container_start_page 371
container_title Journal of medicinal chemistry
container_volume 20
creator Appleton, R. A
Bantick, J. R
Chamberlain, T. R
Hardern, D. N
Lee, T. B
Pratt, A. D
description 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.
doi_str_mv 10.1021/jm00213a012
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ispartof Journal of medicinal chemistry, 1977-03, Vol.20 (3), p.371-379
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language eng
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source American Chemical Society
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
title Antagonists of slow reacting substance of anaphylaxis. Synthesis of a series of chromone-2-carboxylic acids
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