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.