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Page 1
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: since m. 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
8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
Fersing C, Boudot C, Castera-Ducros C, Pinault E, Hutter S, Paoli-Lombardo R, Primas N, Pedron J, Seguy L, Bourgeade-Delmas S, Sournia-Saquet A, Stigliani JL, Brossas JY, Paris L, Valentin A, Wyllie S, Fairlamb AH, Boutet-Robinet É, Corvaisier S, Since M, Malzert-Fréon A, Destere A, Mazier D, Rathelot P, Courtioux B, Azas N, Verhaeghe P, Vanelle P. Fersing C, et al. Among authors: since m. Eur J Med Chem. 2020 Sep 15;202:112558. doi: 10.1016/j.ejmech.2020.112558. Epub 2020 Jul 8. Eur J Med Chem. 2020. PMID: 32652409
Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties.
Fersing C, Boudot C, Paoli-Lombardo R, Primas N, Pinault E, Hutter S, Castera-Ducros C, Kabri Y, Pedron J, Bourgeade-Delmas S, Sournia-Saquet A, Stigliani JL, Valentin A, Azqueta A, Muruzabal D, Destere A, Wyllie S, Fairlamb AH, Corvaisier S, Since M, Malzert-Fréon A, Di Giorgio C, Rathelot P, Azas N, Courtioux B, Vanelle P, Verhaeghe P. Fersing C, et al. Among authors: since m. Eur J Med Chem. 2020 Nov 15;206:112668. doi: 10.1016/j.ejmech.2020.112668. Epub 2020 Aug 4. Eur J Med Chem. 2020. PMID: 32795774
Synthesis of antiplasmodial 2-aminothieno[3,2-d]pyrimidin-4(3H)-one analogues using the scaffold hopping strategy.
Mustière R, Lagardère P, Hutter S, Dell'Orco V, Amanzougaghene N, Tajeri S, Franetich JF, Corvaisier S, Since M, Malzert-Fréon A, Masurier N, Lisowski V, Verhaeghe P, Mazier D, Azas N, Vanelle P, Primas N. Mustière R, et al. Among authors: since m. Eur J Med Chem. 2022 Nov 5;241:114619. doi: 10.1016/j.ejmech.2022.114619. Epub 2022 Jul 20. Eur J Med Chem. 2022. PMID: 35872545
Nongenotoxic 3-Nitroimidazo[1,2-a]pyridines Are NTR1 Substrates That Display Potent in Vitro Antileishmanial Activity.
Fersing C, Basmaciyan L, Boudot C, Pedron J, Hutter S, Cohen A, Castera-Ducros C, Primas N, Laget M, Casanova M, Bourgeade-Delmas S, Piednoel M, Sournia-Saquet A, Belle Mbou V, Courtioux B, Boutet-Robinet É, Since M, Milne R, Wyllie S, Fairlamb AH, Valentin A, Rathelot P, Verhaeghe P, Vanelle P, Azas N. Fersing C, et al. Among authors: since m. ACS Med Chem Lett. 2018 Dec 19;10(1):34-39. doi: 10.1021/acsmedchemlett.8b00347. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655943 Free PMC article.
New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi.
Pedron J, Boudot C, Brossas JY, Pinault E, Bourgeade-Delmas S, Sournia-Saquet A, Boutet-Robinet E, Destere A, Tronnet A, Bergé J, Bonduelle C, Deraeve C, Pratviel G, Stigliani JL, Paris L, Mazier D, Corvaisier S, Since M, Malzert-Fréon A, Wyllie S, Milne R, Fairlamb AH, Valentin A, Courtioux B, Verhaeghe P. Pedron J, et al. Among authors: since m. ACS Med Chem Lett. 2020 Feb 6;11(4):464-472. doi: 10.1021/acsmedchemlett.9b00566. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292551 Free PMC article.
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: since m. Pharmaceuticals (Basel). 2022 Aug 13;15(8):998. doi: 10.3390/ph15080998. Pharmaceuticals (Basel). 2022. PMID: 36015146 Free PMC article.
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT6 receptor antagonist with therapeutic interest in Alzheimer's disease.
Toublet FX, Lalut J, Hatat B, Lecoutey C, Davis A, Since M, Corvaisier S, Freret T, Sopková-de Oliveira Santos J, Claeysen S, Boulouard M, Dallemagne P, Rochais C. Toublet FX, et al. Among authors: since m. Eur J Med Chem. 2021 Jan 15;210:113059. doi: 10.1016/j.ejmech.2020.113059. Epub 2020 Dec 3. Eur J Med Chem. 2021. PMID: 33310288
29 results