1-SUBSTITUTED 2-BENZYLAMINOBENZIMIDAZOLE DERIVATIVES - COMPOUNDS WITH H-1-ANTIHISTAMINIC ACTIVITY

被引：8

作者：

DASETTIMO, A ^{[1
]}

PRIMOFIORE, G ^{[1
]}

DASETTIMO, F ^{[1
]}

CALZOLARI, L ^{[1
]}

CAZZULANI, P ^{[1
]}

PASSONI, A ^{[1
]}

TOFANETTI, O ^{[1
]}

机构：

[1] BOEHRINGER MANNHEIM ITALIA SPA, RES LABS, I-20052 MONZA, ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 27卷 / 04期

关键词：

2-BENZYLAMINOBENZIMIDAZOLE; H-1-ANTIHISTAMINIC ACTIVITY; INVITRO HISTAMINE; METACHOLINE AND SEROTONIN ANTAGONISM; INVIVO PCA AND HISTAMINE-INDUCED VASOPERMEABILITY INHIBITION;

D O I：

10.1016/0223-5234(92)90153-R

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The preparation of 1-substituted 2-benzylaminobenzimidazole derivatives 13-24 is described. Although these compounds have a different structure from the general structure I of antihistamines, they showed some antihistaminic activity (pA2:5-7) when tested in vitro on guinea pig ileum. The introduction of an additional basic centre as in the Mannich bases 25-27 did not cause any improvement of activity. All the compounds tested proved to be inactive in in vivo induced passive cutaneous anaphylaxis (PCA) and cutaneous vasopermeability in rats.

引用

页码：395 / 400

页数：6

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