| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371088 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
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.
Graphical abstractSix 7-benzylamino-1-isoquinolinamines 2 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.Figure optionsDownload full-size imageDownload as PowerPoint slide
