Mayence, A. and Vanden Eynde J. J., and Kaiser, M. and Brun, R. and Yarlett, N. and Huang, T. L.. (2011) Bis(oxyphenylene)benzimidazoles: a novel class of anti-Plasmodium falciparum agents. Bioorganic & medicinal chemistry : a Tetrahedron publication for the rapid dissemenination of full original research papers and critical reviews on biomolecular chemistry, medicinal chemistry and related disciplines, 19 (24). pp. 7493-7500.
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Official URL: http://edoc.unibas.ch/dok/A6002127
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Abstract
A small library of 26 2,2'-[alkane-alpha,omega-diylbis(oxyphenylene)]bis-1H-benzimidazoles has been prepared and evaluated against Giardia intestinalis, Entamoeba histolytica, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum. Among the tested compounds, eight derivatives (17, 19, 20, 24, 27, 30, 32 and 35) exhibited an anti-Plasmodium falciparum activity characterized by IC(50) values in the range of 180-410nM (0.11-0.21mug/mL) and selectivity indexes (IC(50) rat skeletal myoblasts L6 cells vs IC(50)P. falciparum K1 strain) varying between 92 and more than 450. Two of the eight novel drug leads, namely compounds 19 and 32, were also active against G. intestinalis and L. donovani with selectivity indexes of 122 and <164 respectively
| 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 and Kaiser, Marcel |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Pergamon |
| ISSN: | 0968-0896 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
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| Last Modified: | 08 Dec 2017 13:59 |
| Deposited On: | 08 Nov 2012 16:09 |
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