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Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI

Farahat, Abdelbasset A. and Bennett-Vaughn, Cheree and Mineva, Ekaterina M. and Kumar, Arvind and Wenzler, Tanja and Brun, Reto and Liu, Yang and Wilson, W. David and Boykin, David W.. (2016) Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI. Bioorganic & medicinal chemistry letters, 26 (24). pp. 5907-5910.

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Official URL: http://edoc.unibas.ch/53604/

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Abstract

A series of novel benzimidazole diamidines were prepared from the corresponding dicyano analogues either by applying Pinner methodology (5a-c, 10 and 13a) or by making amidoximes intermediates that were reduced to the corresponding amidines (15a-c). The new amidines were evaluated in vitro against the protozoan parasite Trypanosoma brucei rhodesiense (T. b. r.). The thiophene analogue 5b and the N-methyl compound 15a showed superior antitrypanosomal activity compared to that of the parent I.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wenzler, Tanja and Brun, Reto and Kumar, Ashish
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Pergamon
ISSN:0960-894X
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:20 Apr 2017 12:29
Deposited On:20 Apr 2017 12:29

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