2. Academic Validation
  3. Synthesis and antiparasitic and antifungal evaluation of 2'-arylsubstituted-1H,1'H-[2,5']bisbenzimidazolyl-5-carboxamidines

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

  • Eur J Med Chem. 2009 May;44(5):2002-8. doi: 10.1016/j.ejmech.2008.10.003.
Mehmet Alp 1,  Hakan Göker,  Reto Brun,  Sulhiye Yildiz
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.
PMID: 19010569 DOI: 10.1016/j.ejmech.2008.10.003
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.

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