Bakunov, S. A. and Bakunova, S. M. and Wenzler, T. and Ghebru, M. and Werbovetz, K. A. and Brun, R. and Tidwell, R. R.. (2010) Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles. Journal of Medicinal Chemistry, 53 (1). pp. 254-272.
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Official URL: http://edoc.unibas.ch/dok/A5843032
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Abstract
Novel dicationic triazoles 1-60 were synthesized by the Pinner method from the corresponding dinitriles, prepared via the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC). The type and the placement of cationic moieties as well as the nature of aromatic substituents influenced in vitro antiprotozoal activities of compounds 1-60 against Trypanosoma brucei rhodesiense, Plasmodium falciparum, and Leishmania donovani and their cytotoxicity for mammalian cells. Eight congeners displayed antitrypanosomal IC50 values below 10 nM. Thirty-nine dications were more potent against P.falciparum than pentamidine (IC50 = 58 nM), and eight analogues were more active than artemisinin (IC50 = 6 W). Diimidazoline 60 exhibited antiplasmodial IC50 value of 0.6 W. Seven congeners administered at 4 x 5 mg/kg by the intraperitoneal route cured at least three out of four animals in the acute mouse model of African trypanosomiasis. At 4 x 1 mg/kg, diamidine 46 displayed better antitrypanosomal efficacy than melarsoprol, curing all infected mice
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) |
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UniBasel Contributors: | Brun, Reto |
Item Type: | Article, refereed |
Article Subtype: | Research Article |
Publisher: | American Chemical Society |
ISSN: | 0022-2623 |
Note: | Publication type according to Uni Basel Research Database: Journal article |
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Identification Number: |
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Last Modified: | 13 Sep 2018 14:23 |
Deposited On: | 08 Jun 2012 06:47 |
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