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Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2023

Novel thienopyrimidones targeting hepatic and erythrocytic stages of Plasmodium parasites with increased microsomal stability

Nicolas Primas

Résumé

Based on the structure of a previously identified hit, Gamhepathiopine 1, which showed promising antiplasmodial activity, but poor microsomal stability, several strategies were investigated to improve the metabolic stability of the compounds. This included the introduction of fluorine or deuterium atoms, as well as carbocyclic groups. Among the new compounds, the 2-aminocyclobutyl derivative 5g demonstrated enhanced microsomal stability compared to compound 1, while retaining antiplasmodial activity against erythrocytic and hepatic stages of Plasmodium, without significant cytotoxicity against primary hepatocytes.

Domaines

Chimie
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mercredi 5 juin 2024
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Dates et versions

hal-04503282 , version 1 (13-03-2024)

Identifiants

Citer

Prisca Lagardère, Romain Mustière, Nadia Amanzougaghene, Sébastien Hutter, Marion Casanova, et al.. Novel thienopyrimidones targeting hepatic and erythrocytic stages of Plasmodium parasites with increased microsomal stability. European Journal of Medicinal Chemistry, 2023, 261, pp.115873. ⟨10.1016/j.ejmech.2023.115873⟩. ⟨hal-04503282⟩
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