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喹啉-2-羧酸四环衍生物的抗过敏活性。2. 一些苯并噻吩并喹啉羧酸。

Antiallergic activity of tetracyclic derivatives of quinoline-2-carboxylic acid. 2. Some benzothienoquinolinecarboxylic acids.

作者信息

Wade J J, Erickson E H, Hegel R F, Lappi L R, Rice T K

出版信息

J Med Chem. 1978 Sep;21(9):941-8. doi: 10.1021/jm00207a018.

Abstract

Some benzothienoquinolinecarboxylic acids were synthesized and tested in the rat passive cutaneous anaphylaxis (PCA) assay as potential antiallergic agents. Many of the compounds showed activity comparable to that shown by disodium cromoglycate (DSFG); two of them, 1,4-dihydro-4,6,6-trioxo-5-chloro[1]benzothieno[2,3-g]quinoline-2-carboxylic acid and 1,4-dihydro-1,7-dioxo[1]benzothieno[3,2-f]quinoline-3-carboxylic acid, showed potency approximately eightfold greater than that of DSCG in the PCA assay.

摘要

合成了一些苯并噻吩并喹啉羧酸,并在大鼠被动皮肤过敏反应(PCA)试验中作为潜在的抗过敏剂进行了测试。许多化合物表现出与色甘酸二钠(DSFG)相当的活性;其中两种化合物,1,4-二氢-4,6,6-三氧代-5-氯[1]苯并噻吩并[2,3-g]喹啉-2-羧酸和1,4-二氢-1,7-二氧代[1]苯并噻吩并[3,2-f]喹啉-3-羧酸,在PCA试验中的效力比DSCG高约八倍。

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