Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Activity of Amidine-containing Diphenylureas Against P. falciparum

Author(s): Guatam Bhattacharya, Lucia Gerena, Suping Jiang, Karl A. Werbovetz.

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

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Article Details

VOLUME: 2
ISSUE: 2
Year: 2005
Page: [162 - 164]
Pages: 3
DOI: 10.2174/1570180053175061
Price: $58