Karaaslan, Cigdem and Kaiser, Marcel and Brun, Reto and Göker, Hakan. (2016) Synthesis and potent antiprotozoal activity of mono/di amidino 2-anilinobenz-imidazoles versus Plasmodium falciparum and Trypanosoma brucei rhodesiense. Bioorganic and Medicinal Chemistry, 24 (18). pp. 4038-4044.
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Abstract
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.
| Faculties and Departments: | 09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser) |
|---|---|
| UniBasel Contributors: | Brun, Reto and Kaiser, Marcel |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Elsevier |
| ISSN: | 0968-0896 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Language: | English |
| edoc DOI: | |
| Last Modified: | 18 Sep 2017 10:48 |
| Deposited On: | 17 Nov 2016 11:40 |
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