title: In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones.
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.
authors.affiliation: Department of Chemistry, United States Naval Academy, Annapolis, MD 21402, USA. gutterid@usna.edu
authors.forename: Clare E
authors.initials: CE
authors.lastname: Gutteridge
authors.forename: Marshall M
authors.initials: MM
authors.lastname: Hoffman
authors.forename: Apurba K
authors.initials: AK
authors.lastname: Bhattacharjee
authors.forename: Wilbur K
authors.initials: WK
authors.lastname: Milhous
authors.forename: Lucia
authors.initials: L
authors.lastname: Gerena
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry* / Q000494:pharmacology*; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology*; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000737:chemistry / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy; D008958:Models, Molecular; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D047188:Chalcones; D002738:Chloroquine