FN Archimer Export Format
PT J
TI Alkoxyamines Designed as Potential Drugs against Plasmodium and Schistosoma Parasites
BT 
AF 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
AS 1:1,2;2:3;3:1,2;4:1,2;5:1;6:1;7:1;8:1;9:1,2;10:3;11:4;12:3;13:3;14:5;15:1;16:1,2,6;17:3;
FF 1:;2:;3:;4:;5:;6:;7:;8:;9:;10:;11:;12:;13:;14:;15:;16:;17:;
C1 Laboratoire de Chimie de Coordination du CNRS, LCC-CNRS, Université de Toulouse, CNRS, 31555 Toulouse, France
   Institut de Pharmacologie et de Biologie Structurale, IPBS, Université de Toulouse, CNRS, UPS, 31077 Toulouse, France
   Aix Marseille University, CNRS, ICR, UMR 7273, Case 551, Avenue Escadrille Normandie-Niemen, 13397 Marseille CEDEX 20, France
   S.A.S ParaDev, 52 Avenue Paul Alduy, 66860 Perpignan, France
   Laboratoire Interactions Hôtes-Pathogènes-Environnements (IHPE), UMR 5244 CNRS, University of Perpignan, IFREMER, Univ. Montpellier, F-66860 Perpignan, France
   INSERM, Institut National de la Santé et de la Recherche Médicale, 31024 Toulouse, France
C2 UNIV TOULOUSE, FRANCE
   UNIV TOULOUSE, FRANCE
   UNIV AIX MARSEILLE, FRANCE
   S.A.S PARADEV, FRANCE
   CNRS, FRANCE
   INSERM, FRANCE
UM IHPE
IN WOS Cotutelle UMR
   DOAJ
   copubli-france
   copubli-univ-france
IF 0.182
TC 9
UR https://archimer.ifremer.fr/doc/00648/76024/76920.pdf
   https://archimer.ifremer.fr/doc/00648/76024/76921.pdf
LA English
DT Article
DE ;alkoxyamine;alkylation;heme;malaria;radical chemistry;schistosomiasis
AB 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 chemical starting points of the series for improvement of the activity, and further structure activity, relationship studies. Moreover, investigation of the mode of action and the rate constants kd for C-ON bond homolysis of new alkoxyamines is reported, showing a possible alkyl radical mediated biological activity. A theoretical chemistry study allowed us to design new structures of alkoxyamines in order to improve the selectivity index of these drugs 
PY 2020
PD SEP
SO Molecules
SN 1420-3049
PU MDPI AG
VL 25
IS 17
UT 000569607900001
DI 10.3390/molecules25173838
ID 76024
ER

EF