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

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

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Publications

2023
2022

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

Useful links

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Address

Laboratoire de chimie de coordination du CNRS

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

+ 33 5 61 33 31 00