New antimalarial molecules and pharmacological approaches (Team V)

LCC

Overview

Our work, combining chemistry and biology, is based on different pharmacological approaches such as the understanding of:

1) the mechanisms of resistance of pathogens to drugs, and

2) the mode of action of molecules of therapeutic interest.

These studies lead to the design, synthesis, evaluation and mechanistic studies of drug candidates for the treatment of pathologies in which transition metals are involved such as malaria, Alzheimer’s disease, etc… Our team is also labelled Inserm (ERL 1289, MAAP).

Members of the team

All
Responsable d’équipe, Directrice de recherche Inserm, HDR

BENOIT-VICAL Françoise

Doctorante

ABID Imen

Chercheur invité CNRS

AUGEREAU Jean-Michel

Directeur de recherche CNRS, HDR

BALTAS Michel

CACHET Nadja
chercheur invité

CACHET Nadja

Master 2

GUICHONNET Maxime

Post-doc

GUIMARAES Marco

Master 2

HARB Jana

KADRI Naka
Master 2

KADRI Naka

Doctorante

KOUMPOURA Christina

LAURENT Marion
Doctorante

LAURENT Marion

Doctorante

MANARANCHE Jeanne

MARCHOU Bruno
Professeur des Universités - Praticien hospitalier, HDR

MARCHOU Bruno

Directeur de recherche CNRS émérite, HDR

MEUNIER Bernard

Researcher

NARDELLA Flore

Research engineer

NGUYEN Michel

Chargée de recherche CNRS, HDR

PALOQUE Lucie

ROBERT Anne
Directeur de recherche CNRS, HDR

ROBERT Anne

SACRAMENTO Adrielle
Guest

SACRAMENTO Adrielle

Doctorante

SALIM Maryam

SAULNIER Steve
CDD

SAULNIER Steve

Master 2

TRESSIERES Roxane

Master 2

URRUTIA Maider

No Results Found

Responsable d’équipe, Directrice de recherche Inserm, HDR

BENOIT-VICAL Françoise

Equipe V

Après une formation en Parasitologie (option Maladies tropicales) et un doctorat en Biologie-Santé (1997), F. Benoit-Vical a travaillé sur la valorisation de la médecine traditionnelle dans le traitement du paludisme et sur le mode d’action de l’artémisinine. Elle a bénéficié d’un contrat d’interface Inserm-Hôpitaux de Toulouse et a été conseillère scientifique de la spin-off PALUMED SA pour le développement d’antipaludiques. Dans le cadre de nouvelles approches pharmacologiques, F. Benoit-Vical s’intéresse aux mécanismes de résistance de Plasmodium falciparum et aux travaux de pharmaco-modulation en chimie médicinale à visée antipaludique afin de proposer de nouvelles solutions thérapeutiques.

Email:francoise.benoit-vical(at)lcc-toulouse.fr

Téléphone:05.61.17.58.23

Numéro ORCID:0000-0002-9468-4823

Bureau:IPBS A-1B

Equipe:V

Doctorante

ABID Imen

Email:imen.abid(at)lcc-toulouse.fr

Téléphone:05.61.33.31.21

Bureau:B021

Equipe:V

Chercheur invité CNRS

AUGEREAU Jean-Michel

Equipe V

Email:jean-michel.augereau(at)lcc-toulouse.fr

Téléphone:05.61.17.58.31

Numéro ORCID:0000-0002-2847-1969

Bureau:IPBS A-1C

Equipe:V

Directeur de recherche CNRS, HDR

BALTAS Michel

Equipe V

Email:michel.baltas(at)lcc-toulouse.fr

Téléphone:05.61.33.31.38

Bureau:B021

Equipe:V

chercheur invité

CACHET Nadja

Email:nadja.cachet(at)lcc-toulouse.fr

Téléphone:05.61.33.31.39

Bureau:B016

Equipe:V

Master 2

GUICHONNET Maxime

Email:maxime.guichonnet(at)lcc-toulouse.fr

Tel:05.61.33.31.12

Bureau:C018

Equipe:V

Post-doc

GUIMARAES Marco

Email:marco.guimaraes(at)lcc-toulouse.fr

Téléphone:05.61.33.31.12

Bureau:C18

Equipe:V

Master 2

HARB Jana

Email:jana.harb(at)lcc-toulouse.fr

Téléphone:05.61.33.31.38

bureau:B106

Equipes:G et V

Master 2

KADRI Naka

Email:naka.kadri(at)lcc-toulouse.fr

Téléphone:05.61.33.31.38

Bureau:B021

Equipe:V

Doctorante

KOUMPOURA Christina

Email:christina.koumpoura(at)lcc-toulouse.fr

Téléphone:05.61.33.31.12

Bureau:C018

Equipe:V

Doctorante

LAURENT Marion

Email:marion.laurent(at)lcc-toulouse.fr

Téléphone:05.61.17.58.69

Bureau:IPBS

Equipe:V

Doctorante

MANARANCHE Jeanne

Email:jeanne.manaranche(at)lcc-toulouse.fr

Téléphone:05.61.17.58.69

Bureau:IPBS

Equipe:V

Professeur des Universités - Praticien hospitalier, HDR

MARCHOU Bruno

Equipe V

Email:bruno.marchou(at)lcc-toulouse.fr

Téléphone:05.61.77.20.49

Numéro ORCID:0000-0002-0673-2945

Bureau:CHU

Equipe:V

Directeur de recherche CNRS émérite, HDR

MEUNIER Bernard

Equipe V

Email:bernard.meunier(at)lcc-toulouse.fr

Téléphone:05.61.33.31.84

Numéro ORCID:0000-0003-2200-7142

Bureau:B152

Equipe:V

Researcher

NARDELLA Flore

Email:flore.nardella(at)lcc-toulouse.fr

Phone:05.61.17.58.69

Office:IPBS

Team:V

Research engineer

NGUYEN Michel

Equipe V

Email:michel.nguyen(at)lcc-toulouse.fr

Téléphone:05.61.33.31.12

Numéro ORCID:0000-0002-6496-0495

Bureau:C18 / IPBS A-3B

Equipe:V

Chargée de recherche CNRS, HDR

PALOQUE Lucie

Equipe V

Lucie Paloque est parasitologue et a obtenu son doctorat en 2013 à l’Université d’Aix-Marseille pour la recherche de nouvelles cibles thérapeutiques et l’identification de candidats médicaments dans le traitement des leishmanioses. Elle poursuit ces recherches lors d’un premier post-doctorat à l’Université Paul Sabatier. En 2015 elle intègre le LCC comme post-doctorante, pour développer de nouvelles approches pharmacologiques dans le traitement du paludisme, puis y est recrutée en 2019.

Email:lucie.paloque(at)lcc-toulouse.fr

Téléphone:05.61.17.58.69

Numéro ORCID:0000-0003-0359-3959

Bureau:IPBS A-1C

Equipe:V

Directeur de recherche CNRS, HDR

ROBERT Anne

Equipe V

Anne Robert. Ingénieur ENSCT, PhD (1985), HDR (1995), Chargé de recherche CNRS (1985). Actuellement Directeur de recherche CNRS. Oxydations biomimétiques; rôle des métaux rédox en biologie. Mécanisme d’action des peroxydes antipaludiques (artémisinine) et nouveaux antipaludiques ciblant l’hème; régulateurs de l’homéostasie du cuivre comme candidats-médicaments contre la maladie d’Alzheimer.

Email:anne.robert(at)lcc-toulouse.fr

Téléphone:05.61.33.31.26

Numéro ORCID:0000-0002-9092-6776

Bureau:C22

Equipe:V

Guest

SACRAMENTO Adrielle

Email:adrielle.sacramento(at)lcc-toulouse.fr

Phone:05.61.17.58.69

Office:IPBS

Team:V

Doctorante

SALIM Maryam

Email:maryam.salim(at)lcc-toulouse.fr

Téléphone:05.61.17.58.69

Bureau:IPBS

Equipe:V

CDD

SAULNIER Steve

Email:steve.saulnier(at)lcc-toulouse.fr

Phone:05.61.33.31.12

Office:C018

Team:V

Master 2

TRESSIERES Roxane

Email:roxane.tressieres(at)lcc-toulouse.fr

Téléphone:05.61.17.58.31

Bureau:IPBS

Equipe:V

Master 2

URRUTIA Maider

Email:maider.urrutia(at)lcc-toulouse.fr

Phone:05.61.17.58.69

Office:IPBS

Team:V

Research topics

Mechanisms of Plasmodium resistance and therapeutic targets

Markers of resistance selection

Mechanochemical approaches for the synthesis of antimalarial molecules

Alzheimer disease

Team news

Publications

2024

Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents
Guan Y., Nguyen M., Robert A., Liu Y., Meunier B.
RSC Medicinal Chemistry 2024,
http://dx.doi.org/10.1039/D4MD00171K
https://hal.science/hal-04606276

Unprecedented linear products by a mechanochemically activated Biginelli reaction using lawsone
Koumpoura C. L., Vendier L., Bijani C., Robert A., Carbonnière P., Sotiropoulos J.-M., Baltas M.
RSC Mechanochemistry 2024, 1(2), 167-175.
http://dx.doi.org/10.1039/D3MR00032J
https://hal.science/hal-04550806

The synthesis of 2′-hydroxychalcones under ball mill conditions and their biological activities
Abid I., Moslah W., Cojean S., Imbert N., Loiseau P. M., Chamayou A., Srairi-Abid N., Calvet R., Baltas M.
Molecules 2024, 29(8), 1819/1-20.
https://doi.org/10.3390/molecules29081819
https://hal.science/hal-04550832

Hybrid peptide-alkoxyamine drugs: A strategy for the development of a new family of antiplasmodial drugs
Embo-Ibouanga A. W., Nguyen M., Paloque L., Coustets M., Joly J.-P., Augereau J.-M., Vanthuyne N., Bikanga R., Coquin N., Robert A., Audran G., Boissier J., Mellet P., Benoit-Vical F., Marque S. R. A.
Molecules 2024, 29 (6), 1397/1-19.
https://doi.org/10.3390/molecules29061397
https://hal.science/hal-04515160

Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum
Reyser T., Paloque L., Augereau J.-M., Di Stefano L., Benoit-Vical F.
Malaria Journal 2024, 23 (1), 44/1-18.
https://doi.org/10.1186/s12936-024-04855-9
https://hal.science/hal-04502290

Synthesis of novel artemisinin, ciprofloxacin, and norfloxacin hybrids with potent antiplasmodial activity
Vamvoukaki G., Antoniou A. I., Baltas M., Mouray E., Charneau S., Grellier P., Athanassopoulos C. M.
Antibiotics 2024, 13 (2), 142/1-22.
https://doi.org/10.3390/antibiotics13020142
https://hal.science/hal-04509679

2023

The specific copper(II) chelator TDMQ20 is efficient for the treatment of Wilson’s disease in mice
Zhu Y., Tang Y., Huang L., Nguyen M., Liu Y., Robert A., Meunier B.
Pharmaceutics 2023, 15(12), 2719/1-15.
https://doi.org/10.3390/pharmaceutics15122719
https://hal.science/hal-04322010

Epidrugs as promising tools to eliminate Plasmodium falciparum artemisinin-resistant and quiescent parasites
Reyser T., Paloque L., Nguyen M., Augereau J.-M., Fuchter M. J., Lopez M. J., Arimondo P. B., Hassell-Hart S., Spencer J., Di Stefano L., Benoit-Vical F.
Pharmaceutics 2023, 15(10), 2440/1-15.
https://doi.org/10.3390/pharmaceutics15102440
https://hal.science/hal-04269105

Design, synthesis and evaluation of novel pyrimidinylaminothiophene derivatives as FGFR1 inhibitors against human glioblastoma multiforme
Li Y.-L., Yan L.-J., Chen H.-X., Ruan B.-K., Dao P., Du Z.-Y., Dong C.-Z., Meunier B.
European Journal of Medicinal Chemistry 2023, 260, 115764/1-13.
https://doi.org/10.1016/j.ejmech.2023.115764
https://hal.science/hal-04209922

Hybrid molecules based on an emodin scaffold. Synthesis and activity against SARS-CoV-2 and Plasmodium
Li Y., Touret F., de Lamballerie X., Nguyen M., Laurent M., Benoit-Vical F., Robert A., Liu Y., Meunier B.
Organic & Biomolecular Chemistry 2023, 21(36), 7382-7394.
http://dx.doi.org/10.1039/D3OB01122D
https://hal.science/hal-04201757

Mechanochemical studies on coupling of hydrazines and hydrazine amides with phenolic and furanyl aldehydes-hydrazones with antileishmanial and antibacterial activities
Kapusterynska A., Bijani C., Paliwoda D., Vendier L., Bourdon V., Imbert N., Cojean S., Loiseau P. M., Recchia D., Scoffone V. C., Degiacomi G., Akhir A., Saxena D., Chopra S., Lubenets V., Baltas M.
Molecules 2023, 28(13), 5284/1-26.
https://doi.org/10.3390/molecules28135284
https://hal.science/hal-04157067

Oxidation of TDMQ20, a specific copper Chelator as potential drug against Alzheimer’s disease
Nguyen M., Li Y., Robert A., Liu Y., Meunier B.
ChemistrySelect 2023, 8(8), e202204877/1-8.
https://doi.org/10.1002/slct.202204877
https://hal.science/hal-04007798

2022

Distribution in rat blood and brain of TDMQ20, a copper chelator designed as a drug-candidate for Alzheimer’s disease
Huang L., Zeng Y., Li Y., Zhu Y., He Y., Liu Y., Robert A., Meunier B.
Pharmaceutics 2022, 14(12), 2691/1-13.
https://doi.org/10.3390/pharmaceutics14122691
https://hal.science/hal-03985553

Proteomics evidence of the role of TDMQ20 in the cholinergic system and synaptic transmission in a mouse model of Alzheimer’s disease
Sun F., Zhao J., Zhang H., Shi Q., Liu Y., Robert A., Liu Q., Meunier B.
ACS Chemical Neuroscience 2022, 13(21), 3093–3107.
https://doi.org/10.1021/acschemneuro.2c00455
https://hal.archives-ouvertes.fr/hal-03826219

Design of anti-infectious agents from lawsone in a three-component reaction with aldehydes and isocyanides
Koumpoura C. L., Nguyen M., Bijani C., Vendier L., Salina E. G., Buroni S., Degiacomi G., Cojean S., Loiseau P. M., Benoit-Vical F., García-Sosa A. T., Robert A., Baltas M.
ACS Omega 2022, 7(40), 35635-35655.
https://doi.org/10.1021/acsomega.2c03421
https://hal.archives-ouvertes.fr/hal-03818601

In vitro and in silico antimalarial evaluation of FM-AZ, a new artemisinin derivative
Tsamesidis I., Mousavizadeh F., Egwu C. O., Amanatidou D., Pantaleo A., Benoit-Vical F., Reybier K., Giannis A.
Medicines 2022, 9(2), 8/1-12.
https://doi.org/10.3390/medicines9020008
https://hal.archives-ouvertes.fr/hal-03660647

How to define a nanozyme
Robert A., Meunier B.
ACS Nano 2022, 16(5), 6956-6959.
https://doi.org/10.1021/acsnano.2c02966
https://hal.archives-ouvertes.fr/hal-03681945

Mutation in the Plasmodium falciparum BTB/POZ domain of K13 protein confers artemisinin resistance
Paloque L., Coppée R., Stokes B. H., Gnädig N. F., Niaré K., Augereau J.-M., Fidock D. A., Clain J., Benoit-Vical F.
Antimicrobial Agents and Chemotherapy 2022, 66(1), e01320-21.
https://doi.org/10.1128/AAC.01320-21
https://hal.archives-ouvertes.fr/hal-03561782

X-Ray diffraction structure of Cu(II) and Zn(II) complexes of 8-aminoquinoline derivatives (TDMQ), related to the activity of these chelators as potential drugs against Alzheimer’s disease
Li Y., Nguyen M., Vendier L., Robert A., Liu Y., Meunier B.
Journal of Molecular Structure 2022, 1251, 132078/1-6.
https://doi.org/10.1016/j.molstruc.2021.132078
https://hal.archives-ouvertes.fr/hal-03509314

Synthesis and antimalarial activities of new hybrid Atokel molecules
Li Y., Loureiro A., Nguyen M., Laurent M., Bijani C., Benoit-Vical F., Robert A., Liu Y., Meunier B.
ChemistryOpen 2022, 11(5), e202200064/1-20.
https://doi.org/10.1002/open.202200064
https://hal.archives-ouvertes.fr/hal-03681793

Resistance to artemisinin in falciparum malaria parasites: A redox-mediated phenomenon
Egwu C. O., Pério P., Augereau J.-M., Tsamesidis I., Benoit-Vical F., Reybier K.
Free Radical Biology and Medicine 2022, 179, 317-327.
https://doi.org/10.1016/j.freeradbiomed.2021.08.016
https://hal.archives-ouvertes.fr/hal-03561900

2021

TDMQ20, a specific copper chelator, reduces memory impairments in Alzheimer’s disease mouse models
Zhao J., Shi Q., Tian H., Li Y., Liu Y., Xu Z., Robert A., Liu Q., Meunier B.
ACS Chemical Neuroscience 2021, 12(1), 140-149.
https://doi.org/10.1021/acschemneuro.0c00621
https://hal.archives-ouvertes.fr/hal-03079460

Novel molecule combinations and corresponding hybrids targeting artemisinin-resistant Plasmodium falciparum parasites
Ouji M., Nguyen M., Mustière R., Jimenez T., Augereau J.-M., Benoit-Vical F., Deraeve C.
Bioorganic & Medicinal Chemistry Letters 2021, 39, 127884/1-6.
https://doi.org/10.1016/j.bmcl.2021.127884
https://hal.archives-ouvertes.fr/hal-03170976

Antimalarial inhibitors targeting epigenetics or mitochondria in Plasmodium falciparum: Recent survey upon synthesis and biological evaluation of potential drugs against malaria
Koumpoura C. L., Robert A., Athanassopoulos C. M., Baltas M.
Molecules 2021, 26(18), 5711/1-34.
https://doi.org/10.3390/molecules26185711
https://hal.archives-ouvertes.fr/hal-03366266

Elucidation of the Diels-Alder reaction kinetics between diphenylfulvene and maleimide by mechanochemistry and in solution
Gonnet L., Chamayou A., André-Barrès C., Micheau J.-C., Guidetti B., Sato T., Baron M., Baltas M., Calvet R.
ACS Sustainable Chemistry & Engineering 2021, 9(12), 4453-4462.
https://doi.org/10.1021/acssuschemeng.0c08314
https://hal.archives-ouvertes.fr/hal-03197711

Synthesis of biologically relevant 1,2,3- and 1,3,4-triazoles: From classical pathway to green chemistry
Gonnet L., Baron M., Baltas M.
Molecules 2021, 26(18), 5667/1-27.
https://doi.org/10.3390/molecules26185667
https://hal.archives-ouvertes.fr/hal-03360993

Superoxide: A major role in the mechanism of action of essential antimalarial drugs
Egwu C. O., Tsamesidis I., Pério P., Augereau J.-M., Benoit-Vical F., Reybier K.
Free Radical Biology and Medicine 2021, 167, 271-275.
https://doi.org/10.1016/j.freeradbiomed.2021.03.001
https://hal.archives-ouvertes.fr/hal-03203905

Reactive oxygen species as the brainbox in malaria treatment
Egwu C. O., Augereau J.-M., Reybier K., Benoit-Vical F.
Antioxidants 2021, 10(12), 1872/1-20.
https://doi.org/10.3390/antiox10121872
https://hal.archives-ouvertes.fr/hal-03542736

A new thienopyrimidinone chemotype shows multistage activity against Plasmodium falciparum, including artemisinin-resistant parasites
Bosson-Vanga H., Primas N., Franetich J.-F., Lavazec C., Gomez L., Ashraf K., Tefit M., Soulard V., Dereuddre-Bosquet N., Le Grand R., Donnette M., Mustière R., Amanzougaghene N., Tajeri S., Suzanne P., Malzert-Fréon A., Rault S., Vanelle P., Hutter S., Cohen A., Snounou G., Roques P., Azas N., Lagardère P., Lisowski V., Masurier N., Nguyen M., Paloque L., Benoit-Vical F., Verhaeghe P., Mazier D., Muralidharan V.
Microbiology Spectrum 2021, 9(2), e00274-21/1-19.
https://doi.org/10.1128/Spectrum.00274-21
https://hal.archives-ouvertes.fr/hal-03363796

2-phenoxy-3-trichloromethylquinoxalines are antiplasmodial aerivatives with activity against the apicoplast of Plasmodium falciparum
Amrane D., Arnold C.-S., Hutter S., Sanz-Serrano J., Collia M., Azqueta A., Paloque L., Cohen A., Amanzougaghene N., Tajeri S., Franetich J.-F., Mazier D., Benoit-Vical F., Verhaeghe P., Azas N., Vanelle P., Botté C., Primas N.
Pharmaceuticals 2021, 14(8), 724/1-24.
https://doi.org/10.3390/ph14080724
https://hal.archives-ouvertes.fr/hal-03323862

“Nanozymes” without catalytic activity should be renamed
[Unpublished work], 2021
Nguyen M., Robert A., Meunier B.
https://hal.archives-ouvertes.fr/hal-03290323

Partnerships

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Alumnae

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Youzhi Li (PhD 2019-2022): post-doc position, Hong-Kong

Chinedu Egwu (PhD 2018-2021): Professor assistant, FUNAI University, Nigeria

Thibaud Reyser (PhD 2017-2020): Technical Service Scientist, Merck KGaA

Manel Ouji (PhD 2017-2020): Medical Information Officer, Pfizer

Sokhna Keita Alassane (PhD 2013-2016)

Arba Pramundita Ramadani (PhD 2013-2017): Professor Assistant, Department of Pharmacy Yogyakarta, Indonesia

Gallery

The haemozoin crystals (produced by the parasite’s digestion of haemoglobin) move under the effect of light.

Useful links

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LCC

Laboratoire de chimie de coordination du CNRS

205 route de Narbonne, BP 44099
31077 Toulouse cedex 4
France

+ 33 5 61 33 31 00