Synthesis and potent antiprotozoal activity of mono/di amidino 2-anilinobenzimidazoles versus Plasmodium falciparum and Trypanosoma brucei rhodesiense

Karaaslan C., Kaiser M., Brun R., GÖKER A. H.

BIOORGANIC & MEDICINAL CHEMISTRY, cilt.24, sa.18, ss.4038-4044, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 24 Sayı: 18
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1016/j.bmc.2016.06.047
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.4038-4044
  • Anahtar Kelimeler: Anilinobenzimidazoles, Carboxamidines, Antiparasitic agents, Plasmodium falciparum, Trypanosoma brucei rhodesiense, DERIVATIVES, ANTIFUNGAL, DISEASES, BINDING, AGENTS
  • Ankara Üniversitesi Adresli: Evet

Özet

A series of mono and dicationic new 2-anilinobenzimidazole carboxamidines were prepared in a four step process starting from 4-amino-3-nitrobenzonitrile and corresponding o-phenylenediamines. Their antiparasitic activity against Plasmodium falciparum (P. falciparum) and Trypanosoma brucei rhodesiense (T. b. rhodesiense) were evaluated in vitro. Some of the dicationic compounds (10,12,14) showed equal or very close activity against T. b. rhodesiense with melarsoprol and also showed promising activity against P. falciparum as compared to chloroquine. Among the monocationic derivatives compound 21 exhibited best inhibitory activity against P. falciparum. (C) 2016 Elsevier Ltd. All rights reserved.