| Literature DB >> 26638044 |
Paula F Carneiro1, Maria C R F Pinto1, Roberta K F Marra2, Fernando de C da Silva2, Jackson A L C Resende3, Luiz F Rocha E Silva4, Hilkem G Alves5, Gleyce S Barbosa5, Marne C de Vasconcellos5, Emerson S Lima5, Adrian M Pohlit4, Vitor F Ferreira6.
Abstract
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.Entities:
Keywords: Epoxides; Infectious disease; Lapachone; Malaria; Naphthoquinones
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Year: 2015 PMID： 26638044 DOI： 10.1016/j.ejmech.2015.11.020
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514