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, cilt.44, sa.5, ss.2002-2008, 2009 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 44 Sayı: 5
  • Basım Tarihi: 2009
  • Doi Numarası: 10.1016/j.ejmech.2008.10.003
  • Dergi Adı: European Journal of Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.2002-2008
  • Anahtar Kelimeler: Bisbenzimidazoles, Carboxamidine, Antiparasitic agents, Antifungal agents, ANTIMICROBIAL AGENTS, DIGUANIDINO, DISEASES, BENZIMIDAZOLES, ANTIPROTOZOAL, LEISHMANIASIS, DERIVATIVES, DISCOVERY
  • Lokman Hekim Üniversitesi Adresli: Hayır

Özet

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.