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| Reyser, Thibaud; To, Tung H.; Egwu, Chinedu; Paloque, Lucie; Nguyen, Michel; Hamouy, Alexandre; Stigliani, Jean-luc; Bijani, Christian; Augereau, Jean-michel; Joly, Jean-patrick; Portela, Julien; Havot, Jeffrey; Marque, Sylvain R. A.; Boissier, Jérôme; Robert, Anne; Benoit-vical, Françoise; Audran, Gérard. |
| Malaria and schistosomiasis are major infectious causes of morbidity and mortality in the tropical and sub-tropical areas. Due to the widespread drug resistance of the parasites, the availability of new efficient and affordable drugs for these endemic pathologies is now a critical public health issue. In this study, we report the design, the synthesis and the preliminary biological evaluation of a series of alkoxyamine derivatives as potential drugs against Plasmodium and Schistosoma parasites. The compounds (RS/SR)-2F, (RR/SS)-2F, and 8F, having IC50 values in nanomolar range against drug-resistant P. falciparum strains, but also five other alkoxyamines, inducing the death of all adult worms of S. mansoni in only 1 h, can be considered as interesting... |
| Tipo: Text |
Palavras-chave: Alkoxyamine; Alkylation; Heme; Malaria; Radical chemistry; Schistosomiasis. |
| Ano: 2020 |
URL: https://archimer.ifremer.fr/doc/00648/76024/76920.pdf |
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