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Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines

Farahat, A. A. and Kumar, A. and Say, M. and Barghash Aedm, and Goda, F. E. and Eisa, H. M. and Wenzler, T. and Brun, R. and Liu, Y. and Mickelson, L. and Wilson, W. D. and Boykin, D. W.. (2010) Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines. Bioorganic & Medicinal Chemistry, 18 (2). pp. 557-566.

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Official URL: http://edoc.unibas.ch/dok/A5843033

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Abstract

A novel series of extended DAPI analogues were prepared by insertion of either a carbon-carbon triple bond (16a-d) or a phenyl group (21a, b and 24) at position-2. The new amidines were evaluated in vitro against both Trypanosoma brucei rhodesiense (T. b. r.) and Plasmodium falciparum (P. f.). Five compounds (16a, 16b, 16d, 21a, 21b) exhibited IC50 values against T. b. r. of 9 nM or less which is two to nine folds more effective than DAPI. The same five compounds exhibited IC50 values against P. f. of 5.9 nM or less which is comparable to that of DAPI. The fluorescence properties of these new molecules were recorded, however; they do not offer any advantage over those of DAPI. (C) 2009 Elsevier Ltd. All rights reserved
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto
Item Type:Article, refereed
Bibsysno:Link to catalogue
Publisher:Pergamon
ISSN:0968-0896
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:07 Nov 2017 08:16
Deposited On:08 Jun 2012 06:47

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