NOVEL BENZOTHIOPHENECARBOXAMIDOTETRAZOLE, BENZOFURANCARBOXAMIDOTETRAZOLE, AND NAPHTHALENECARBOXAMIDOTETRAZOLE AS POTENTIAL ANTIALLERGY AGENTS

被引:76
作者
CONNOR, DT [1 ]
CETENKO, WA [1 ]
MULLICAN, MD [1 ]
SORENSON, RJ [1 ]
UNANGST, PC [1 ]
WEIKERT, RJ [1 ]
ADOLPHSON, RL [1 ]
KENNEDY, JA [1 ]
THUESON, DO [1 ]
WRIGHT, CD [1 ]
CONROY, MC [1 ]
机构
[1] WARNER LAMBERT PARKE DAVIS,DIV PARKE DAVIS PHARMACEUT RES,DEPT PHARMACOL,ANN ARBOR,MI 48105
关键词
D O I
10.1021/jm00083a023
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and antiallergic activity of a series of novel benzothiophene-, benzofuran-, and naphthalenecarbox-amidotetrazoles are described. A number of the compounds inhibit the release of histamine from anti-IgE stimulated basophils obtained from allergic donors. Optimal inhibition is exhibited in benzothiophenes with a 3-alkoxy substituent in combination with a 5-methoxy, 6-methoxy, or a 5,6-dimethoxy group. Compounds 13c (CI-959) also inhibited respiratory burst of human neutrophils and the release of mediators from anti-IgE-stimulated human chopped lung.
引用
收藏
页码:958 / 965
页数:8
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