Publication date: Available online 25 June 2016
Source:Bioorganic & Medicinal Chemistry
Author(s): Cigdem Karaaslan, Marcel Kaiser, Reto Brun, Hakan Göker
A series of mono and dicationic new 2-anilinobenz- imidazole carboxamidines were prepared in a four step process starting from 4- amino-3nitrobenzonitrile 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.
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