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New imidazolidinedione derivatives as antimalarial agents. | LitMetric

New imidazolidinedione derivatives as antimalarial agents.

Bioorg Med Chem

Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, United States.

Published: February 2011

AI Article Synopsis

Article Abstract

A series of new N-alky- and N-alkoxy-imidazolidinediones was prepared and assessed for prophylactic and radical curative activities in mouse and Rhesus monkey models. New compounds are generally metabolically stable, weakly active in vitro against Plasmodium falciparum clones (D6 and W2) and in mice infected with Plasmodium berghei sporozoites. Representative compounds 8e and 9c showed good causal prophylactic activity in Rhesus monkeys dosed 30 mg/kg/day for 3 consecutive days by IM, delayed patency for 19-21 days and 54-86 days, respectively, as compared to the untreated control. By oral, 9c showed only marginal activity in causal prophylactic and radical curative tests at 50 mg/kg/day×3 and 30 mg/kg/day×7 plus chloroquine 10 mg/kg for 7 days, respectively.

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Source
http://dx.doi.org/10.1016/j.bmc.2010.12.028DOI Listing

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