A Chemically Stable Fluorescent Mimic of Dihydroartemisinin, Artemether, and Arteether with Conserved Bioactivity and Specificity Shows High Pharmacological Relevance to the Antimalarial Drugs.

Antimalarials / pharmacology Artemether Artemisinins / pharmacology
Plasmodium artemisinin drugs fluorescent imaging stability

Journal

ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580

Informations de publication

Date de publication:
10 07 2020
Historique:
pubmed: 9 4 2020
medline: 24 6 2021
entrez: 9 4 2020
Statut: ppublish

Résumé

Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i.e., dihydroartemisinin, artemether, arteether, and artemisone) were synthesized from dihydroartemisinin. One of these tracers, corresponding to a dihydroartemisinin/artemether/arteether mimic, showed a combination of excellent physicochemical and biological properties such as hydrolytic stability, high inhibitory potency against blood-stage parasites, similar ring-stage survival assay values than the clinical antimalarials, high cytopermeability and specific labeling of live

Identifiants

DOI: 10.1021/acsinfecdis.9b00430 PMID: 32267151
pubmed: 32267151
doi: 10.1021/acsinfecdis.9b00430
doi:

Substances chimiques

Antimalarials 0
Artemisinins 0
artenimol 6A9O50735X
Artemether C7D6T3H22J
artemotil XGL7GFB9YI

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1532-1547

Auteurs

Abdoulaye Sissoko (A)

Université de Paris, MERIT, IRD, F-75006 Paris, France.
Laboratoire d'Excellence GR-Ex, Paris, France.

Pedro Vásquez-Ocmín (P)

Université Paris-Saclay, CNRS, BioCIS, F-92290 Châtenay-Malabry, France.

Alexandre Maciuk (A)

Université Paris-Saclay, CNRS, BioCIS, F-92290 Châtenay-Malabry, France.

Daniela Barbieri (D)

Laboratoire d'Excellence GR-Ex, Paris, France.
Université de Paris, U1016, INSERM, and UMR 8104, CNRS, F-75014 Paris, France.

Gaëlle Neveu (G)

Laboratoire d'Excellence GR-Ex, Paris, France.
Université de Paris, U1016, INSERM, and UMR 8104, CNRS, F-75014 Paris, France.

Laurine Rondepierre (L)

Université de Paris, MERIT, IRD, F-75006 Paris, France.
Laboratoire d'Excellence GR-Ex, Paris, France.

Raphaël Grougnet (R)

Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.

Pascale Leproux (P)

Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.

Magali Blaud (M)

Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.

Karim Hammad (K)

Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.

Sylvie Michel (S)

Université de Paris, CiTCoM, CNRS, F-75006 Paris, France.

Catherine Lavazec (C)

Laboratoire d'Excellence GR-Ex, Paris, France.
Université de Paris, U1016, INSERM, and UMR 8104, CNRS, F-75014 Paris, France.

Jérôme Clain (J)

Université de Paris, MERIT, IRD, F-75006 Paris, France.
Laboratoire d'Excellence GR-Ex, Paris, France.

Sandrine Houzé (S)

Université de Paris, MERIT, IRD, F-75006 Paris, France.
CNR du Paludisme, AP-HP, Hôpital Bichat - Claude-Bernard, F-75018 Paris, France.

Romain Duval (R)

Université de Paris, MERIT, IRD, F-75006 Paris, France.
Laboratoire d'Excellence GR-Ex, Paris, France.
ORCID: 0000-0002-0125-506X

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiparasitaires › Antiprotozoaires › Antipaludiques › A Chemically Stable Fluorescent Mimic of...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Terpènes › Sesquiterpènes › Artémisinines › Artéméther › A Chemically Stable Fluorescent Mimic of...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Terpènes › Sesquiterpènes › Artémisinines › A Chemically Stable Fluorescent Mimic of...