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Novel thienopyrimidones targeting hepatic and erythrocytic stages of Plasmodium parasites with increased microsomal stability.
Lagardère P, Mustière R, Amanzougaghene N, Hutter S, Casanova M, Franetich JF, Tajeri S, Malzert-Fréon A, Corvaisier S, Since M, Azas N, Vanelle P, Verhaeghe P, Primas N, Mazier D, Masurier N, Lisowski V. Lagardère P, et al. Among authors: verhaeghe p. Eur J Med Chem. 2023 Dec 5;261:115873. doi: 10.1016/j.ejmech.2023.115873. Epub 2023 Oct 13. Eur J Med Chem. 2023. PMID: 37857143
New antiplasmodial 4-amino-thieno[3,2-d]pyrimidines with improved intestinal permeability and microsomal stability.
Lagardère P, Mustière R, Amanzougaghene N, Hutter S, Casanova M, Franetich JF, Tajeri S, Malzert-Fréon A, Corvaisier S, Azas N, Vanelle P, Verhaeghe P, Primas N, Mazier D, Masurier N, Lisowski V. Lagardère P, et al. Among authors: verhaeghe p. Eur J Med Chem. 2023 Mar 5;249:115115. doi: 10.1016/j.ejmech.2023.115115. Epub 2023 Jan 13. Eur J Med Chem. 2023. PMID: 36680984
Target fishing reveals PfPYK-1 and PfRab6 as potential targets of an antiplasmodial 4-anilino-2-trichloromethylquinazoline hit compound.
Kieffer C, Primas N, Hutter S, Merckx A, Reininger L, Bach S, Ruchaud S, Gaillard F, Laget M, Amrane D, Hervé L, Castera-Ducros C, Renault J, Dumètre A, Rault S, Doerig C, Rathelot P, Vanelle P, Azas N, Verhaeghe P. Kieffer C, et al. Among authors: verhaeghe p. Bioorg Med Chem. 2024 Mar 15;102:117654. doi: 10.1016/j.bmc.2024.117654. Epub 2024 Feb 28. Bioorg Med Chem. 2024. PMID: 38452406
Improving Aqueous Solubility and In Vitro Pharmacokinetic Properties of the 3-Nitroimidazo[1,2-a]pyridine Antileishmanial Pharmacophore.
Paoli-Lombardo R, Primas N, Bourgeade-Delmas S, Hutter S, Sournia-Saquet A, Boudot C, Brenot E, Castera-Ducros C, Corvaisier S, Since M, Malzert-Fréon A, Courtioux B, Valentin A, Verhaeghe P, Azas N, Rathelot P, Vanelle P. Paoli-Lombardo R, et al. Among authors: verhaeghe p. Pharmaceuticals (Basel). 2022 Aug 13;15(8):998. doi: 10.3390/ph15080998. Pharmaceuticals (Basel). 2022. PMID: 36015146 Free PMC article.
Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interest of the salicylanilide pharmacophore in the fight against tuberculosis.
Le NH, Constant P, Tranier S, Nahoum V, Guillet V, Maveyraud L, Daffé M, Mourey L, Verhaeghe P, Marrakchi H. Le NH, et al. Among authors: verhaeghe p. Bioorg Med Chem. 2022 Oct 1;71:116938. doi: 10.1016/j.bmc.2022.116938. Epub 2022 Jul 29. Bioorg Med Chem. 2022. PMID: 35933838 Free article.
4-Substituted Thieno[3,2-d]pyrimidines as Dual-Stage Antiplasmodial Derivatives.
Lagardère P, Mustière R, Amanzougaghene N, Hutter S, Franetich JF, Azas N, Vanelle P, Verhaeghe P, Primas N, Mazier D, Masurier N, Lisowski V. Lagardère P, et al. Among authors: verhaeghe p. Pharmaceuticals (Basel). 2022 Jul 1;15(7):820. doi: 10.3390/ph15070820. Pharmaceuticals (Basel). 2022. PMID: 35890119 Free PMC article.
229 results