Abstract
Amidine-containing derivatives of the diphenylurea antimalarial lead compound WR268961, a putative plasmepsin inhibitor, were prepared and tested against erythrocyte-stage P. falciparum. Diamidine 8 was the most active compound, displaying IC50 values of 54 nM and 41 nM versus chloroquine sensitive (D6) and chloroquine resistant (W2) parasites, respectively.
Keywords: diamidine, antimalarial, plasmodium falciparum, plasmepsin, heme assembly
Letters in Drug Design & Discovery
Title: Activity of Amidine-containing Diphenylureas Against P. falciparum
Volume: 2 Issue: 2
Author(s): Guatam Bhattacharya, Lucia Gerena, Suping Jiang and Karl A. Werbovetz
Affiliation:
Keywords: diamidine, antimalarial, plasmodium falciparum, plasmepsin, heme assembly
Abstract: Amidine-containing derivatives of the diphenylurea antimalarial lead compound WR268961, a putative plasmepsin inhibitor, were prepared and tested against erythrocyte-stage P. falciparum. Diamidine 8 was the most active compound, displaying IC50 values of 54 nM and 41 nM versus chloroquine sensitive (D6) and chloroquine resistant (W2) parasites, respectively.
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Cite this article as:
Bhattacharya Guatam, Gerena Lucia, Jiang Suping and Werbovetz A. Karl, Activity of Amidine-containing Diphenylureas Against P. falciparum, Letters in Drug Design & Discovery 2005; 2 (2) . https://dx.doi.org/10.2174/1570180053175061
DOI https://dx.doi.org/10.2174/1570180053175061 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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