Exploiting a basic chemosensitizing pharmacophore hypothesis. Part 1: synthesis and biological evaluation of novel arylbromide and bicyclic chemosensitizers against drug-resistant malaria parasites.
An exploratory series of novel arylbromide and bicyclic chemosensitizers (modulators) against chloroquine-resistant Plasmodium falciparum were designed and synthesized on the basis of a basic chemosensitizing pharmacophore hypothesis in malaria. ortho-Substituted bromo and biphenyl ether compounds displayed the best activity from the series.
Chouteau
Franck
F
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Ramanitrahasimbola
David
D
Rasoanaivo
Philippe
P
Chibale
Kelly
K
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D018432:Drug Resistance, Multiple; D006801:Humans; D006842:Hydrocarbons, Brominated / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008288:Malaria / Q000097:blood / Q000188:drug therapy* / Q000469:parasitology; D010640:Phenothiazines / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014966:Xanthenes / Q000737:chemistry
D000962:Antimalarials; D019086:Bridged Bicyclo Compounds, Heterocyclic; D006842:Hydrocarbons, Brominated; D010640:Phenothiazines; D014966:Xanthenes; D002738:Chloroquine; C031637:phenothiazine