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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. Pharmaceuticals (Basel). 2022 Aug 13;15(8):998. doi: 10.3390/ph15080998. Pharmaceuticals (Basel). 2022. PMID: 36015146 Free PMC article.
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: paoli lombardo r. 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: paoli lombardo r. 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