Activity of Amidine-containing Diphenylureas Against P. falciparum

Guatam Bhattacharya; Lucia Gerena; Suping Jiang; Karl A. Werbovetz

doi:10.2174/1570180053175061

ISSN: 1570-1808
E-ISSN: 1875-628X

Activity of Amidine-containing Diphenylureas Against P. falciparum
Authors: Guatam Bhattacharya¹, Lucia Gerena², Suping Jiang³ and Karl A. Werbovetz⁴
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¹ Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA. ² Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA. ³ Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA. ⁴ Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA.
Source: Letters in Drug Design & Discovery, Volume 2, Issue 2, Mar 2005, p. 162 - 164
DOI: https://doi.org/10.2174/1570180053175061
- Available online: 01 Mar 2005

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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2005-03-01

2025-05-19

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Article Type: Review Article

Keyword(s): antimalarial; diamidine; heme assembly; plasmepsin; plasmodium falciparum

Activity of Amidine-containing Diphenylureas Against P. falciparum

Abstract

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