In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones.

Department of Chemistry, United States Naval Academy, Annapolis, MD 21402, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.65). 01/2011; 21(2):786-9. DOI: 10.1016/j.bmcl.2010.11.099
Source: PubMed

ABSTRACT A series of 1,7-diaminoisoquinolinamines, that are expected to mediate antimalarial activity by the same mechanism employed by the chalcones, were produced. Six 7-benzylamino-1-isoquinolinamines were found to be submicromolar inhibitors in vitro of drug-resistant Plasmodium falciparum, with the best possessing activity comparable to chloroquine. Despite being developed from a lead that is a DHFR inhibitor, these compounds do not mediate their antimalarial effects by inhibition of DHFR.

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