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Site-selective protein-modification chemistry for basic biology and drug development.
The most exciting current and future applications of chemical site-selective protein modification are highlighted and which hurdles still need to be overcome for more widespread use are considered. Expand
Drug Screen Targeted at Plasmodium Liver Stages Identifies a Potent Multistage Antimalarial Drug
Oral administration of a single dose of decoquinate effectively prevents the appearance of disease and warrants its exploitation as a potent antimalarial compound. Expand
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
A novel series of quinolin-4(1H)-imines as dual-stage antiplasmodials, several-fold more active than primaquine in vitro against Plasmodium berghei liver stage are presented and the compounds are metabolically stable and modulate several drug targets. Expand
Novel Potent Metallocenes against Liver Stage Malaria
ABSTRACT Novel conjugates of the antimalarial drug primaquine (compound 1) with ferrocene, named primacenes, have been synthesized and screened for their activities against blood stage and liverExpand
Flavones as isosteres of 4(1H)-quinolones: discovery of ligand efficient and dual stage antimalarial lead compounds.
Ligand efficient leads were identified as dual stage antimalarials, suggesting that scaffold optimization may afford potent antiplasmodial compounds. Expand
Triterpenoids as inhibitors of erythrocytic and liver stages of Plasmodium infections.
Active compounds were shown to inhibit the parasite's intracellular development rather than its ability to invade hepatic cells, and toxicity of compounds 1-6 towards human cells was also investigated, showing that they were not toxic or exhibited weak toxicity. Expand
4-C-Me-DAB and 4-C-Me-LAB - enantiomeric alkyl-branched pyrrolidine iminosugars - are specific and potent α-glucosidase inhibitors; acetone as the sole protecting group.
The effect of pH on the NMR spectra of 4-C-Me-DAB [pK(a) of the salt around 8.4] is discussed and illustrates the need for care in analysis of both coupling constants and chemical shift. Expand
Dual-stage triterpenoids from an African medicinal plant targeting the malaria parasite.
Sixteen triterpenoids (1-16), previously isolated from the aerial parts of the African medicinal plant Momordica balsamina or obtained by derivatization, were evaluated for their activity againstExpand
The title bicyclic lactone, C19H19NO3, is an intermediate in the synthesis of chiral α-methylprolines and branched C-methyl pyrrolidines; the absolute configuration was determined by the use ofExpand