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

ALP M., GÖKER A. H., Brun R., YILDIZ S.

European Journal of Medicinal Chemistry, vol.44, no.5, pp.2002-2008, 2009 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 44 Issue: 5
  • Publication Date: 2009
  • Doi Number: 10.1016/j.ejmech.2008.10.003
  • Journal Name: European Journal of Medicinal Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.2002-2008
  • Keywords: Bisbenzimidazoles, Carboxamidine, Antiparasitic agents, Antifungal agents, ANTIMICROBIAL AGENTS, DIGUANIDINO, DISEASES, BENZIMIDAZOLES, ANTIPROTOZOAL, LEISHMANIASIS, DERIVATIVES, DISCOVERY
  • Lokman Hekim University Affiliated: No

Abstract

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. © 2008 Elsevier Masson SAS. All rights reserved.