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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. Among authors: valentin a. Pharmaceuticals (Basel). 2022 Aug 13;15(8):998. doi: 10.3390/ph15080998. Pharmaceuticals (Basel). 2022. PMID: 36015146 Free PMC article.
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: valentin a. 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.
Antileishmanial pharmacomodulation in 8-nitroquinolin-2(1H)-one series.
Kieffer C, Cohen A, Verhaeghe P, Paloque L, Hutter S, Castera-Ducros C, Laget M, Rault S, Valentin A, Rathelot P, Azas N, Vanelle P. Kieffer C, et al. Among authors: valentin a. Bioorg Med Chem. 2015 May 15;23(10):2377-86. doi: 10.1016/j.bmc.2015.03.064. Epub 2015 Mar 31. Bioorg Med Chem. 2015. PMID: 25846065
Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
Pedron J, Boudot C, Hutter S, Bourgeade-Delmas S, Stigliani JL, Sournia-Saquet A, Moreau A, Boutet-Robinet E, Paloque L, Mothes E, Laget M, Vendier L, Pratviel G, Wyllie S, Fairlamb A, Azas N, Courtioux B, Valentin A, Verhaeghe P. Pedron J, et al. Among authors: valentin a. Eur J Med Chem. 2018 Jul 15;155:135-152. doi: 10.1016/j.ejmech.2018.06.001. Epub 2018 Jun 5. Eur J Med Chem. 2018. PMID: 29885575 Free PMC article.
8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
Fersing C, Boudot C, Pedron J, Hutter S, Primas N, Castera-Ducros C, Bourgeade-Delmas S, Sournia-Saquet A, Moreau A, Cohen A, Stigliani JL, Pratviel G, Crozet MD, Wyllie S, Fairlamb A, Valentin A, Rathelot P, Azas N, Courtioux B, Verhaeghe P, Vanelle P. Fersing C, et al. Among authors: valentin a. Eur J Med Chem. 2018 Sep 5;157:115-126. doi: 10.1016/j.ejmech.2018.07.064. Epub 2018 Aug 1. Eur J Med Chem. 2018. PMID: 30092366 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: valentin a. 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.
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: valentin a. 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: valentin a. 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
Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium.
Cohen A, Suzanne P, Lancelot JC, Verhaeghe P, Lesnard A, Basmaciyan L, Hutter S, Laget M, Dumètre A, Paloque L, Deharo E, Crozet MD, Rathelot P, Dallemagne P, Lorthiois A, Sibley CH, Vanelle P, Valentin A, Mazier D, Rault S, Azas N. Cohen A, et al. Among authors: valentin a. Eur J Med Chem. 2015 May 5;95:16-28. doi: 10.1016/j.ejmech.2015.03.011. Epub 2015 Mar 10. Eur J Med Chem. 2015. PMID: 25791675
Antitrypanosomatid Pharmacomodulation at Position 3 of the 8-Nitroquinolin-2(1H)-one Scaffold Using Palladium-Catalysed Cross-Coupling Reactions.
Pedron J, Boudot C, Bourgeade-Delmas S, Sournia-Saquet A, Paloque L, Rastegari M, Abdoulaye M, El-Kashef H, Bonduelle C, Pratviel G, Wyllie S, Fairlamb AH, Courtioux B, Verhaeghe P, Valentin A. Pedron J, et al. Among authors: valentin a. ChemMedChem. 2018 Oct 22;13(20):2217-2228. doi: 10.1002/cmdc.201800456. Epub 2018 Sep 17. ChemMedChem. 2018. PMID: 30221468 Free PMC article.
594 results