Synthesis and antiparasitic and antifungal evaluation of 2′-arylsubstituted-1H,1′H-[2,5′]bisbenzimidazolyl-5-carboxamidines

被引：60
作者：
Alp, Mehmet [1 ]
Goker, Hakan [1 ]
Brun, Reto [2 ]
Yildiz, Sulhiye [3 ]
机构：
[1] Ankara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey
[2] Swiss Trop Inst, CH-4002 Basel, Switzerland
[3] Ankara Univ, Fac Pharm, Dept Microbiol, TR-06100 Ankara, Turkey
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 05期
关键词：
Bisbenzimidazoles; Carboxamidine; Antiparasitic agents; Antifungal agents; ANTIMICROBIAL AGENTS; DIGUANIDINO; DISEASES; BENZIMIDAZOLES; ANTIPROTOZOAL; LEISHMANIASIS; DERIVATIVES; DISCOVERY;
D O I：
10.1016/j.ejmech.2008.10.003
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2'-arylsubstituted-1H,1'H-[2,5']-bisbenzimidazolyl-5-carboxamidines were prepared in a six-step process starting from 4-amino-3-nitrobenzonitrile. The antiparasitic activity against Trypanosoma brucei rhodesiense (T.b.r.), Plasmodium falciparum (P.f.), Leishmania donovani (L.d.) and Trypanosoma cruzi (T.c.) and antifungal activity against Candida albicans and Candida krusei were evaluated in vitro. Several compounds showed promising in vitro activity against T.b.r., P.f and C albicans and had superior activity against P.f. as compared to chloroquine. (C) 2008 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：2002 / 2008
页数：7
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