| Literature DB >> 20031421 |
Abdelbasset A Farahat1, Arvind Kumar, Martial Say, Alaa El-Din M Barghash, Fatma E Goda, Hassan M Eisa, Tanja Wenzler, Reto Brun, Yang Liu, Leah Mickelson, W David Wilson, David W Boykin.
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 IC(50) values against T. b. r. of 9nM or less which is two to nine folds more effective than DAPI. The same five compounds exhibited IC(50) values against P. f. of 5.9nM 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. Copyright 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20031421 DOI： 10.1016/j.bmc.2009.12.011
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641