作为抗过敏剂的（2-羧基-1,4-二氢-4-氧代喹啉基）草氨酸和（2-羧基-1,4-二氢-4-氧代苯并[h]喹啉基）草氨酸

(2-Carboxy-1,4-dihydro-4-oxoquinolyl)oxamic acids and (2-carboxy-1,4-dihydro-4-oxobenzo[h]quinolyl)oxamic acids as antiallergy agents.

作者信息

Wright J B, Johnson H G

出版信息

J Med Chem. 1977 Jan;20(1):166-9. doi: 10.1021/jm00211a038.

Abstract

A group of (2-carboxy-1,4-dihydro-4-oxoquinolyl)oxamic acids (5) containing the oxamic acid group in the 5,6, or 7 positions were synthesized and investigated for antiasthma activity as indicated by the passive cutaneous anaphylaxis (PCA) reaction in rats. Also synthesized and investigated were two (2-carbosy-1,4-dihydro-4-oxobenzo[h]-quinolyl)oxamic acids (9 and 10). Several of the compounds synthesized (viz. 5e, 5f, and 10) showed activity in the PCA test approximately 25 times that shown by disodium cromoglycate (1), as measured by the ID50 doses.

摘要

合成了一组在5、6或7位含有草氨酸基团的（2-羧基-1,4-二氢-4-氧代喹啉基）草氨酸（5），并通过大鼠被动皮肤过敏反应（PCA）研究了其抗哮喘活性。还合成并研究了两种（2-羧基-1,4-二氢-4-氧代苯并[h]喹啉基）草氨酸（9和10）。通过半数抑制剂量（ID50）测定，合成的几种化合物（即5e、5f和10）在PCA试验中的活性约为色甘酸钠（1）的25倍。