The development of new antimalarial therapeutics is necessary to address the increasing resistance to current drugs. Bicyclic azetidines targeting Plasmodium falciparum phenylalanyl-tRNA synthetase comprise one promising new class of antimalarials, especially due to their activities against three stages of the parasite's life cycle, but a lengthy synthetic route to these compounds may affect th...

Following a veterinary and behavioral survey of chimpanzees from a natural population in Uganda, leaf samples of Trichilia rubescens were collected because of the unusual method of ingestion observed. The methanolic crude extract of T. rubescens leaves exhibited significant antimalarial activity in vitro. Bioassay-directed fractionation provided two new limonoids, trichirubines A and B. A great...

Several deep-sea marine invertebrates were collected from hydrothermal vents, seamounts and cold coral assemblages in the North Atlantic Ocean, near the Azores islands. The effect of their lipid crude extracts against two strains of malaria parasite P. falciparum (Dd2 and 3D7) was measured in vitro in order to establish the potential of these invertebrates as new sources for antimalarial compou...

Improving the solubility of polysubstituted 1,4-naphthoquinone derivatives was achieved by introducing nitrogen in two different positions of the naphthoquinone core, at C-5 and at C-8 of menadione through a two-step, straightforward synthesis based on the regioselective hetero-Diels-Alder reaction. The antimalarial and the antischistosomal activities of these polysubstituted aza-1,4-naphthoqui...

The aim of this study was to identify new compounds active against Plasmodium falciparum based on our previous research carried out on 3-phenyl-quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC(50) less than 1 microM against the 3D7 strain. Derivative 1 demonstrated high potency (IC(50)= 0...

background: malaria remains the world’s most devastating human parasitic infection. our goal was to assess the capacity of increasing concentrations of five antimalarial drugs (fansidartm, halfantm, quinine, coartemtm and chloroquine phosphate) to elicit the generation of methemoglobin in three human erythrocyte genotypes (hb aa, hb as and hb ss). materials and methods: spectrophotometric metho...

In an effort to develop new antimalarials, some 1,4 naphthoquinone derivatives were designed on the basis of results of computational studies reported in previous paper, which showed that 2 nd or 3 rd or both position of 1,4 naphthoquinone is most suitable for better antimalarial activity. When the reaction of 1,4 naphthoquinone was performed without a catalyst several secondary products were f...