Synthesis and antihistaminic H1 activity of 1,2,5(6)-trisubstituted benzimidazoles

被引：0
|
作者：
Göker, H
Ayhan-Kilcigil, G
Tunçbilek, M
Kus, C
Ertan, R
Kendi, E
Özbey, S
Fort, M
Garcia, C
Farré, AJ
机构：
[1] Ankara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey
[2] Hacettepe Univ, Dept Engn Phys, TR-06532 Ankara, Turkey
[3] Labs Dr Esteve SA, Dept Pharmacol, Barcelona 08041, Spain
来源：
HETEROCYCLES | 1999年 / 51卷 / 11期
关键词：
D O I：
暂无
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N-1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H-1-antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.
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页码：2561 / 2573
页数：13
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