NOVEL BENZOTHIOPHENECARBOXAMIDOTETRAZOLE, BENZOFURANCARBOXAMIDOTETRAZOLE, AND NAPHTHALENECARBOXAMIDOTETRAZOLE AS POTENTIAL ANTIALLERGY AGENTS
NOVEL BENZOTHIOPHENECARBOXAMIDOTETRAZOLE, BENZOFURANCARBOXAMIDOTETRAZOLE, AND NAPHTHALENECARBOXAMIDOTETRAZOLE AS POTENTIAL ANTIALLERGY AGENTS
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DOI：
10.1021/jm00083a023
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发表时间：
1992-03-06
影响因子：
7.3
通讯作者：
CONROY, MC
中科院分区：
文献类型：
--
作者：
CONNOR, DT;CETENKO, WA;CONROY, MC
介绍了一系列新型苯并噻吩、苯并呋喃和萘卡盒酰胺四唑的合成及其抗过敏活性。许多化合物抑制从过敏供体获得的抗ige刺激的嗜碱性粒细胞释放组胺。3-烷氧基取代基与5-甲氧基、6-甲氧基或5,6-二甲氧基结合的苯并噻吩具有最佳抑制作用。化合物13c （CI-959）还能抑制人中性粒细胞的呼吸爆发和抗ige刺激的人切肺中介质的释放。
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.