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Evaluation of amidoxime derivatives as prodrug candidates of potent bis-cationic antimalarials.

Berger O, Ortial S, Wein S, Denoyelle S, Bressolle F, Durand T, Escale R, Vial HJ, Vo-Hoang Y.

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2203-2207. doi: 10.1016/j.bmcl.2019.06.045. Epub 2019 Jun 24.


Structural determinants of the catalytic mechanism of Plasmodium CCT, a key enzyme of malaria lipid biosynthesis.

Guca E, Nagy GN, Hajdú F, Marton L, Izrael R, Hoh F, Yang Y, Vial H, Vértessy BG, Guichou JF, Cerdan R.

Sci Rep. 2018 Jul 25;8(1):11215. doi: 10.1038/s41598-018-29500-9.


Contribution of the precursors and interplay of the pathways in the phospholipid metabolism of the malaria parasite.

Wein S, Ghezal S, Buré C, Maynadier M, Périgaud C, Vial HJ, Lefebvre-Tournier I, Wengelnik K, Cerdan R.

J Lipid Res. 2018 Aug;59(8):1461-1471. doi: 10.1194/jlr.M085589. Epub 2018 May 31.


High Accumulation and In Vivo Recycling of the New Antimalarial Albitiazolium Lead to Rapid Parasite Death.

Wein S, Taudon N, Maynadier M, Tran Van Ba C, Margout D, Bordat Y, Fraisse L, Wengelnik K, Cerdan R, Bressolle-Gomeni F, Vial HJ.

Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00352-17. doi: 10.1128/AAC.00352-17. Print 2017 Aug.


Hydroxyl Ketone-Based Histone Deacetylase Inhibitors To Gain Insight into Class I HDAC Selectivity versus That of HDAC6.

Traoré MDM, Zwick V, Simões-Pires CA, Nurisso A, Issa M, Cuendet M, Maynadier M, Wein S, Vial H, Jamet H, Wong YS.

ACS Omega. 2017 Apr 30;2(4):1550-1562. doi: 10.1021/acsomega.6b00481. Epub 2017 Apr 20.


Erratum: SC83288 is a clinical development candidate for the treatment of severe malaria.

Pegoraro S, Duffey M, Otto TD, Wang Y, Rösemann R, Baumgartner R, Fehler SK, Lucantoni L, Avery VM, Moreno-Sabater A, Mazier D, Vial HJ, Strobl S, Sanchez CP, Lanzer M.

Nat Commun. 2017 Apr 6;8:15273. doi: 10.1038/ncomms15273. No abstract available.


SC83288 is a clinical development candidate for the treatment of severe malaria.

Pegoraro S, Duffey M, Otto TD, Wang Y, Rösemann R, Baumgartner R, Fehler SK, Lucantoni L, Avery VM, Moreno-Sabater A, Mazier D, Vial HJ, Strobl S, Sanchez CP, Lanzer M.

Nat Commun. 2017 Jan 31;8:14193. doi: 10.1038/ncomms14193.


Synthesis of an Uncharged Tetra-cyclopeptide Acting as a Transmembrane Carrier: Enhanced Cellular and Nuclear Uptake.

Francisco Hilário F, Traoré MD, Zwick V, Berry L, Simões-Pires CA, Cuendet M, Fantozzi N, Pereira de Freitas R, Maynadier M, Wein S, Vial H, Wong YS.

Org Lett. 2017 Feb 3;19(3):612-615. doi: 10.1021/acs.orglett.6b03776. Epub 2017 Jan 20.


Corrigendum: Composite Aromatic Boxes for Enzymatic Transformations of Quaternary Ammonium Substrates.

Nagy GN, Marton L, Contet A, Ozohanics O, Ardelean LM, Révész Á, Vékey K, Irimie FD, Vial H, Cerdan R, Vértessy BG.

Angew Chem Int Ed Engl. 2015 Jul 27;54(31):8866. doi: 10.1002/anie.201505314. No abstract available.


An Atypical Mitochondrial Carrier That Mediates Drug Action in Trypanosoma brucei.

de Macêdo JP, Schumann Burkard G, Niemann M, Barrett MP, Vial H, Mäser P, Roditi I, Schneider A, Bütikofer P.

PLoS Pathog. 2015 May 6;11(5):e1004875. doi: 10.1371/journal.ppat.1004875. eCollection 2015 May.


Plasmodium falciparum CTP:phosphocholine cytidylyltransferase possesses two functional catalytic domains and is inhibited by a CDP-choline analog selected from a virtual screening.

Contet A, Pihan E, Lavigne M, Wengelnik K, Maheshwari S, Vial H, Douguet D, Cerdan R.

FEBS Lett. 2015 Apr 13;589(9):992-1000. doi: 10.1016/j.febslet.2015.03.003. Epub 2015 Mar 13.


Uncovering new structural insights for antimalarial activity from cost-effective aculeatin-like derivatives.

Winkler M, Maynadier M, Wein S, Lespinasse MA, Boumis G, Miele AE, Vial H, Wong YS.

Org Biomol Chem. 2015 Feb 21;13(7):2064-77. doi: 10.1039/c4ob02459a.


A chemical proteomics approach for the search of pharmacological targets of the antimalarial clinical candidate albitiazolium in Plasmodium falciparum using photocrosslinking and click chemistry.

Penarete-Vargas DM, Boisson A, Urbach S, Chantelauze H, Peyrottes S, Fraisse L, Vial HJ.

PLoS One. 2014 Dec 3;9(12):e113918. doi: 10.1371/journal.pone.0113918. eCollection 2014.


Investigating source water Cryptosporidium concentration, species and infectivity rates during rainfall-runoff in a multi-use catchment.

Swaffer BA, Vial HM, King BJ, Daly R, Frizenschaf J, Monis PT.

Water Res. 2014 Dec 15;67:310-20. doi: 10.1016/j.watres.2014.08.055. Epub 2014 Sep 26.


Composite aromatic boxes for enzymatic transformations of quaternary ammonium substrates.

Nagy GN, Marton L, Contet A, Ozohanics O, Ardelean LM, Révész A, Vékey K, Irimie FD, Vial H, Cerdan R, Vértessy BG.

Angew Chem Int Ed Engl. 2014 Dec 1;53(49):13471-6. doi: 10.1002/anie.201408246. Epub 2014 Oct 5. Erratum in: Angew Chem Int Ed Engl. 2015 Jul 27;54(31):8866.


Exploring prodrug approaches for albitiazolium and its analogues.

Peyrottes S, Caldarelli S, Wein S, Perigaud C, Vial H.

Curr Top Med Chem. 2014;14(14):1653-67.


Antimalarial bicyclic peroxides belonging to the G-factor family: mechanistic aspects of their formation and iron (II) induced reduction.

Ruiz J, Azema J, Payrastre C, Baltas M, Tuccio B, Vial H, Andre-Barres C.

Curr Top Med Chem. 2014;14(14):1668-83.


New insight into the mechanism of accumulation and intraerythrocytic compartmentation of albitiazolium, a new type of antimalarial.

Wein S, Tran Van Ba C, Maynadier M, Bordat Y, Perez J, Peyrottes S, Fraisse L, Vial HJ.

Antimicrob Agents Chemother. 2014 Sep;58(9):5519-27. doi: 10.1128/AAC.00040-14. Epub 2014 Jul 7.


Design, synthesis and evaluation of new tricyclic endoperoxides as potential antiplasmodial agents.

Ruiz J, Mallet-Ladeira S, Maynadier M, Vial H, André-Barrès C.

Org Biomol Chem. 2014 Jul 28;12(28):5212-21. doi: 10.1039/c4ob00787e.


Discovery of compounds blocking the proliferation of Toxoplasma gondii and Plasmodium falciparum in a chemical space based on piperidinyl-benzimidazolone analogs.

Saïdani N, Botté CY, Deligny M, Bonneau AL, Reader J, Lasselin R, Merer G, Niepceron A, Brossier F, Cintrat JC, Rousseau B, Birkholtz LM, Cesbron-Delauw MF, Dubremetz JF, Mercier C, Vial H, Lopez R, Maréchal E.

Antimicrob Agents Chemother. 2014 May;58(5):2586-97. doi: 10.1128/AAC.01445-13. Epub 2014 Feb 18.


CRIMALDDI: platform technologies and novel anti-malarial drug targets.

Vial H, Taramelli D, Boulton IC, Ward SA, Doerig C, Chibale K.

Malar J. 2013 Nov 5;12:396. doi: 10.1186/1475-2875-12-396.


Development of the first oral bioprecursors of bis-alkylguanidine antimalarial drugs.

Degardin M, Wein S, Duckert JF, Maynadier M, Guy A, Durand T, Escale R, Vial H, Vo-Hoang Y.

ChemMedChem. 2014 Feb;9(2):300-4. doi: 10.1002/cmdc.201300419. Epub 2014 Jan 8.


A novel live-dead staining methodology to study malaria parasite viability.

Pasini EM, van den Ierssel D, Vial HJ, Kocken CH.

Malar J. 2013 Jun 7;12:190. doi: 10.1186/1475-2875-12-190.


Characterization of choline uptake in Trypanosoma brucei procyclic and bloodstream forms.

Macêdo JP, Schmidt RS, Mäser P, Rentsch D, Vial HJ, Sigel E, Bütikofer P.

Mol Biochem Parasitol. 2013 Jul;190(1):16-22. doi: 10.1016/j.molbiopara.2013.05.007. Epub 2013 Jun 6.


Evolutionary and mechanistic insights into substrate and product accommodation of CTP:phosphocholine cytidylyltransferase from Plasmodium falciparum.

Nagy GN, Marton L, Krámos B, Oláh J, Révész Á, Vékey K, Delsuc F, Hunyadi-Gulyás É, Medzihradszky KF, Lavigne M, Vial H, Cerdan R, Vértessy BG.

FEBS J. 2013 Jul;280(13):3132-48. doi: 10.1111/febs.12282. Epub 2013 May 24.


Flexible synthesis and evaluation of diverse anti-Apicomplexa cyclic peptides.

Traoré M, Mietton F, Maubon D, Peuchmaur M, Hilário FF, Pereira de Freitas R, Bougdour A, Curt A, Maynadier M, Vial H, Pelloux H, Hakimi MA, Wong YS.

J Org Chem. 2013 Apr 19;78(8):3655-75. doi: 10.1021/jo4001492. Epub 2013 Apr 4.


Potent in vivo anti-malarial activity and representative snapshot pharmacokinetic evaluation of artemisinin-quinoline hybrids.

Lombard MC, N'Da DD, Tran Van Ba C, Wein S, Norman J, Wiesner L, Vial H.

Malar J. 2013 Feb 21;12:71. doi: 10.1186/1475-2875-12-71.


New bis-thiazolium analogues as potential antimalarial agents: design, synthesis, and biological evaluation.

Caldarelli SA, El Fangour S, Wein S, Tran van Ba C, Périgaud C, Pellet A, Vial HJ, Peyrottes S.

J Med Chem. 2013 Jan 24;56(2):496-509. doi: 10.1021/jm3014585. Epub 2013 Jan 4.


Biochemical characterization of Plasmodium falciparum CTP:phosphoethanolamine cytidylyltransferase shows that only one of the two cytidylyltransferase domains is active.

Maheshwari S, Lavigne M, Contet A, Alberge B, Pihan E, Kocken C, Wengelnik K, Douguet D, Vial H, Cerdan R.

Biochem J. 2013 Feb 15;450(1):159-67. doi: 10.1042/BJ20121480.


Antimalarial and anticancer activities of artemisinin-quinoline hybrid-dimers and pharmacokinetic properties in mice.

Lombard MC, N'Da DD, Breytenbach JC, Kolesnikova NI, Tran Van Ba C, Wein S, Norman J, Denti P, Vial H, Wiesner L.

Eur J Pharm Sci. 2012 Dec 18;47(5):834-41. doi: 10.1016/j.ejps.2012.09.019. Epub 2012 Oct 13.


A quantitative liquid chromatography tandem mass spectrometry method for metabolomic analysis of Plasmodium falciparum lipid related metabolites.

Vo Duy S, Besteiro S, Berry L, Perigaud C, Bressolle F, Vial HJ, Lefebvre-Tournier I.

Anal Chim Acta. 2012 Aug 20;739:47-55. doi: 10.1016/j.aca.2012.06.016. Epub 2012 Jun 17.


Shifting the paradigm: the putative mitochondrial protein ABCB6 resides in the lysosomes of cells and in the plasma membrane of erythrocytes.

Kiss K, Brozik A, Kucsma N, Toth A, Gera M, Berry L, Vallentin A, Vial H, Vidal M, Szakacs G.

PLoS One. 2012;7(5):e37378. doi: 10.1371/journal.pone.0037378. Epub 2012 May 24.


Choline analogues in malaria chemotherapy.

Peyrottes S, Caldarelli S, Wein S, Périgaud C, Pellet A, Vial H.

Curr Pharm Des. 2012;18(24):3454-66. Review.


Disulfide prodrugs of albitiazolium (T3/SAR97276): synthesis and biological activities.

Caldarelli SA, Hamel M, Duckert JF, Ouattara M, Calas M, Maynadier M, Wein S, Périgaud C, Pellet A, Vial HJ, Peyrottes S.

J Med Chem. 2012 May 24;55(10):4619-28. doi: 10.1021/jm3000328. Epub 2012 May 16.


Evaluation of bis-alkylamidoxime O-alkylsulfonates as orally available antimalarials.

Degardin M, Wein S, Gouni S, Tran Van Ba C, Duckert JF, Durand T, Escale R, Vial H, Vo-Hoang Y.

ChemMedChem. 2012 Jun;7(6):991-1001. doi: 10.1002/cmdc.201200112. Epub 2012 Apr 27.


Transport and pharmacodynamics of albitiazolium, an antimalarial drug candidate.

Wein S, Maynadier M, Bordat Y, Perez J, Maheshwari S, Bette-Bobillo P, Tran Van Ba C, Penarete-Vargas D, Fraisse L, Cerdan R, Vial H.

Br J Pharmacol. 2012 Aug;166(8):2263-76. doi: 10.1111/j.1476-5381.2012.01966.x.


Synthesis and antimalarial activities of a diverse set of triazole-containing furamidine analogues.

Berger O, Kaniti A, van Ba CT, Vial H, Ward SA, Biagini GA, Bray PG, O'Neill PM.

ChemMedChem. 2011 Nov 4;6(11):2094-108. doi: 10.1002/cmdc.201100265. Epub 2011 Sep 8.


Synthesis and antiplasmodial activity of streptocyanine/peroxide and streptocyanine/4-aminoquinoline hybrid dyes.

Maether MP, Bernat V, Maturano M, André-Barrès C, Ladeira S, Valentin A, Vial H, Payrastre C.

Org Biomol Chem. 2011 Nov 7;9(21):7400-10. doi: 10.1039/c1ob06048a. Epub 2011 Sep 7.


PG12, a phospholipid analog with potent antimalarial activity, inhibits Plasmodium falciparum CTP:phosphocholine cytidylyltransferase activity.

González-Bulnes P, Bobenchik AM, Augagneur Y, Cerdan R, Vial HJ, Llebaria A, Ben Mamoun C.

J Biol Chem. 2011 Aug 19;286(33):28940-7. doi: 10.1074/jbc.M111.268946. Epub 2011 Jun 25.


Genetic and transcriptional analysis of phosphoinositide-specific phospholipase C in Plasmodium.

Raabe A, Berry L, Sollelis L, Cerdan R, Tawk L, Vial HJ, Billker O, Wengelnik K.

Exp Parasitol. 2011 Sep;129(1):75-80. doi: 10.1016/j.exppara.2011.05.023. Epub 2011 May 30.


Antiplasmodial properties of acyl-lysyl oligomers in culture and animal models of malaria.

Zaknoon F, Wein S, Krugliak M, Meir O, Rotem S, Ginsburg H, Vial H, Mor A.

Antimicrob Agents Chemother. 2011 Aug;55(8):3803-11. doi: 10.1128/AAC.00129-11. Epub 2011 Jun 6.


Multiple roles for Plasmodium berghei phosphoinositide-specific phospholipase C in regulating gametocyte activation and differentiation.

Raabe AC, Wengelnik K, Billker O, Vial HJ.

Cell Microbiol. 2011 Jul;13(7):955-66. doi: 10.1111/j.1462-5822.2011.01591.x. Epub 2011 Apr 26.


Phosphatidylinositol 3-monophosphate is involved in toxoplasma apicoplast biogenesis.

Tawk L, Dubremetz JF, Montcourrier P, Chicanne G, Merezegue F, Richard V, Payrastre B, Meissner M, Vial HJ, Roy C, Wengelnik K, Lebrun M.

PLoS Pathog. 2011 Feb;7(2):e1001286. doi: 10.1371/journal.ppat.1001286. Epub 2011 Feb 17.


Forming spirocyclohexadienone-oxocarbenium cation species in the biomimetic synthesis of amomols.

Traoré M, Maynadier M, Souard F, Choisnard L, Vial H, Wong YS.

J Org Chem. 2011 Mar 4;76(5):1409-17. doi: 10.1021/jo102414s. Epub 2011 Jan 21.


Symmetrical choline-derived dications display strong anti-kinetoplastid activity.

Ibrahim HM, Al-Salabi MI, El Sabbagh N, Quashie NB, Alkhaldi AA, Escale R, Smith TK, Vial HJ, de Koning HP.

J Antimicrob Chemother. 2011 Jan;66(1):111-25. doi: 10.1093/jac/dkq401. Epub 2010 Nov 14.


Pharmacokinetic properties and metabolism of a new potent antimalarial N-alkylamidine compound, M64, and its corresponding bioprecursors.

Margout D, Gattacceca F, Moarbess G, Wein S, Tran van Ba C, Le Pape S, Berger O, Escale R, Vial HJ, Bressolle FM.

Eur J Pharm Sci. 2011 Jan 18;42(1-2):81-90. doi: 10.1016/j.ejps.2010.10.012. Epub 2010 Nov 2.


Reverse-benzamidine antimalarial agents: design, synthesis, and biological evaluation.

Berger O, Wein S, Duckert JF, Maynadier M, El Fangour S, Escale R, Durand T, Vial H, Vo-Hoang Y.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5815-7. doi: 10.1016/j.bmcl.2010.07.124. Epub 2010 Aug 3.


Phosphatidylinositol 3-phosphate, an essential lipid in Plasmodium, localizes to the food vacuole membrane and the apicoplast.

Tawk L, Chicanne G, Dubremetz JF, Richard V, Payrastre B, Vial HJ, Roy C, Wengelnik K.

Eukaryot Cell. 2010 Oct;9(10):1519-30. doi: 10.1128/EC.00124-10. Epub 2010 Aug 13.


CRIMALDDI: a co-ordinated, rational, and integrated effort to set logical priorities in anti-malarial drug discovery initiatives.

Boulton IC, Nwaka S, Bathurst I, Lanzer M, Taramelli D, Vial H, Doerig C, Chibale K, Ward SA.

Malar J. 2010 Jul 13;9:202. doi: 10.1186/1475-2875-9-202.

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