57182-40-8Relevant academic research and scientific papers
Synthesis and antimalarial activity of quinones and structurally-related oxirane derivatives
Carneiro, Paula F.,Pinto, Maria C.R.F.,Marra, Roberta K.F.,Da Silva, Fernando De C.,Resende, Jackson A.L.C.,Rocha E Silva, Luiz F.,Alves, Hilkem G.,Barbosa, Gleyce S.,De Vasconcellos, Marne C.,Lima, Emerson S.,Pohlit, Adrian M.,Ferreira, Vitor F.
, p. 134 - 140 (2016)
A series of eighteen quinones and structurally-related oxiranes were synthesized and evaluated for in vitro inhibitory activity against the chloroquine-sensitive 3D7 clone of the human malaria parasite Plasmodium falciparum. 2-amino and 2-allyloxynaphthoquinones exhibited important antiplasmodial activity (median inhibitory concentrations (IC50) 10 μM). Oxiranes 6 and 25, prepared respectively by reaction of α-lapachone and tetrachloro-p-quinone with diazomethane in a mixture of ether and ethanol, exhibited the highest antiplasmodial activity and low cytotoxicity against human fibroblasts (MCR-5 cell line). The active compounds could represent a good prototype for an antimalarial lead molecule.
