INHIBITION OF RAT PASSIVE CUTANEOUS ANAPHYLAXIS BY 3-(TETRAZOL-5-YL)QUINOLINES

被引：24

作者：

ERICKSON, EH ^{[1
]}

HAINLINE, CF ^{[1
]}

LENON, LS ^{[1
]}

MATSON, CJ ^{[1
]}

RICE, TK ^{[1
]}

SWINGLE, KF ^{[1
]}

VANWINKLE, M ^{[1
]}

机构：

[1] THREE M CO,DEPT PHARMACOL,RIKER LABS,ST PAUL,MN 55101

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 07期

关键词：

D O I：

10.1021/jm00193a013

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quinoline-3-carboxylic acid (3) was found to have weak oral activity in the rat passive cutaneous (PCA) assay. In an effort to increase activity, the synthesis of structurally related compounds was initiated. This led to substituted 3-(tetrazol-5-yl)quinolines, some of which are equal in potency, when given orally, to doxantrazole. Further work resulted in the synthesis of 4-oxoquinolines, one of which, 8-chloro-1, 4-dihydro-4-oxo-3-(tetrazol-5-yl)quinoline (132), is 33-fold more active than disodium cromoglycate (ip) and 32-fold more active than doxantrazole (po). © 1979, American Chemical Society. All rights reserved.

引用

页码：816 / 823

页数：8

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