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Letters in Drug Design & Discovery

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

DOI: 10.2174/1570180053175061

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Activity of Amidine-containing Diphenylureas Against P. falciparum

Page: [162 - 164] Pages: 3

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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