Structural simplification of the 3‐nitroimidazo[1,2‐a]pyridine antileishmanial pharmacophore: Design, synthesis, and antileishmanial activity of novel 2,4-disubstituted 5-nitroimidazoles

Authors: Paoli-Lombardo Romain, Primas Nicolas, Hutter Sébastien, Castera-Ducros Caroline, Jacquet Inès, Verhaeghe Pierre, Azas Nadine, Rathelot Pascal, Vanelle Patrice

Source: Heterocyclic Communications, Vol 30, Iss 1, Pp 312-25 (2024)

Subject Terms: structural simplification, 5-nitroimidazole, vicarious nucleophilic substitution (vns), tetrakis(dimethylamino)ethylene (tdae), antileishmanial activity, Organic chemistry, QD241-441

File Description: electronic resource

Relation: https://doaj.org/toc/2191-0197

Access URL: https://doaj.org/article/42f0656e44c145f09a7d0e0afbba7a75

Former les équipes de soins d’un CHU multi-sites à la problématique des médicaments à haut risque : utilisation d’un escape game

Alternate Title: Training healthcare teams of a multi-site university hospital on high-alert medication issues: Using an escape room (English)

Authors: Leroux, Pierre ^{a, b}, Castera-Ducros, Caroline ^{a, b}, Conreur, Laurence ^{a, b}, Taleb, Said Ait ^{a, b}, Diack, Adja Fatou ^{a, b}, Cayez, Louise ^{a, b}, Paoli-Lombardo, Romain ^{a, b}, Lamy, Édouard ^{a, b}, Primas, Nicolas ^{a, b}, Curti, Christophe ^{a, b}, Vanelle, Patrice ^{a, b}, Rathelot, Pascal ^{a, *, b}

Source: In Annales Pharmaceutiques Françaises February 2025

2,2 ′ -[2,4-Bis(4-chlorophenyl)cyclobutane-1,3-diyl]bis(8-bromo-6-chloro-3-nitroimidazo[1,2- a ]pyridine).

Authors: Jacquet, Inès¹ (AUTHOR) ines.jacquet@etu.univ-amu.fr, Paoli-Lombardo, Romain^1,2 (AUTHOR) romain.paoli-lombardo@univ-amu.fr, Castera-Ducros, Caroline^1,2 (AUTHOR) caroline.ducros@univ-amu.fr, Vanelle, Patrice^1,2 (AUTHOR) patrice.vanelle@univ-amu.fr, Primas, Nicolas^1,2 (AUTHOR) patrice.vanelle@univ-amu.fr

Source: Molbank. Dec2024, Vol. 2024 Issue 4, pM1916. 7p.

Subject Terms: *X-ray crystallography, *MOLECULAR structure, *PYRIDINE derivatives, *RING formation (Chemistry), *PYRIDINE

DprE1 and Ddn as promising therapeutic targets in the development of novel anti-tuberculosis nitroaromatic drugs

Authors: Paoli-Lombardo, Romain, Primas, Nicolas, Vanelle, Patrice

Source: In European Journal of Medicinal Chemistry 5 August 2024 274

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

Authors: Fersing, Cyril, Boudot, Clotilde, Paoli-Lombardo, Romain, Primas, Nicolas, Pinault, Emilie, Hutter, Sébastien, Castera-Ducros, Caroline, Kabri, Youssef, Pedron, Julien, Bourgeade-Delmas, Sandra, Sournia-Saquet, Alix, Stigliani, Jean-Luc, Valentin, Alexis, Azqueta, Amaya, Muruzabal, Damián, Destere, Alexandre, Wyllie, Susan, Fairlamb, Alan H., Corvaisier, Sophie, Since, Marc, Malzert-Fréon, Aurélie, Di Giorgio, Carole, Rathelot, Pascal, Azas, Nadine, Courtioux, Bertrand, Vanelle, Patrice, Verhaeghe, Pierre

Source: In European Journal of Medicinal Chemistry 15 November 2020 206

8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi

Authors: Fersing, Cyril, Boudot, Clotilde, Castera-Ducros, Caroline, Pinault, Emilie, Hutter, Sébastien, Paoli-Lombardo, Romain, Primas, Nicolas, Pedron, Julien, Seguy, Line, Bourgeade-Delmas, Sandra, Sournia-Saquet, Alix, Stigliani, Jean-Luc, Brossas, Jean-Yves, Paris, Luc, Valentin, Alexis, Wyllie, Susan, Fairlamb, Alan H., Boutet-Robinet, Élisa, Corvaisier, Sophie, Since, Marc, Malzert-Fréon, Aurélie, Destere, Alexandre, Mazier, Dominique, Rathelot, Pascal, Courtioux, Bertrand, Azas, Nadine, Verhaeghe, Pierre, Vanelle, Patrice

Source: In European Journal of Medicinal Chemistry 15 September 2020 202

N -[1-(2-Chlorophenyl)-2-{1-methyl-5-nitro-4-[(phenylsulfonyl)methyl]-1 H -imidazol-2-yl}ethyl]-4-methylbenzenesulfonamide.

Authors: Paoli-Lombardo, Romain¹ (AUTHOR) romain.paoli-lombardo@etu.univ-amu.fr, Primas, Nicolas^1,2 (AUTHOR) caroline.ducros@univ-amu.fr, Castera-Ducros, Caroline^1,2 (AUTHOR) pascal.rathelot@univ-amu.fr, Jacquet, Inès¹ (AUTHOR), Rathelot, Pascal^1,2 (AUTHOR), Vanelle, Patrice^1,2 (AUTHOR) nicolas.primas@univ-amu.fr

Source: Molbank. Jun2023, Vol. 2023 Issue 2, pM1633. 5p.

Subject Terms: *CARBANIONS, *MOIETIES (Chemistry), *HYDROGEN, *ETHYLENE, *SULFONES

6-Chloro-3-nitro-8-(phenylthio)-2-[(phenylthio)methyl] imidazo[1,2- a ]pyridine.

Authors: Paoli-Lombardo, Romain¹ (AUTHOR) romain.paoli-lombardo@etu.univ-amu.fr, Primas, Nicolas^1,2 (AUTHOR) caroline.ducros@univ-amu.fr, Hutter, Sébastien³ (AUTHOR) sebastien.hutter@univ-amu.fr, Bourgeade-Delmas, Sandra⁴ (AUTHOR) sandra.bourgeade-delmas@ird.fr, Boudot, Clotilde⁵ (AUTHOR) bertrand.courtioux@unilim.fr, Castera-Ducros, Caroline^1,2 (AUTHOR) ines.jacquet@etu.univ-amu.fr, Jacquet, Inès¹ (AUTHOR) pascal.rathelot@univ-amu.fr, Courtioux, Bertrand⁵ (AUTHOR), Azas, Nadine³ (AUTHOR) nadine.azas@univ-amu.fr, Rathelot, Pascal^1,2 (AUTHOR), Vanelle, Patrice^1,2 (AUTHOR) nicolas.primas@univ-amu.fr

Source: Molbank. Jun2023, Vol. 2023 Issue 2, pM1613. 6p.

Subject Terms: *PYRIDINE, *STRUCTURE-activity relationships, *CELL survival, *CELL lines, *PROMASTIGOTE

6-Chloro-3-nitro-2-[(phenylsulfonyl)methyl]imidazo[1,2- b ]pyridazine.

Authors: Paoli-Lombardo, Romain¹ (AUTHOR), Primas, Nicolas^1,2 (AUTHOR) nicolas.primas@univ-amu.fr, Hutter, Sébastien³ (AUTHOR), Bourgeade-Delmas, Sandra⁴ (AUTHOR), Boudot, Clotilde⁵ (AUTHOR), Castera-Ducros, Caroline^1,2 (AUTHOR), Jacquet, Inès¹ (AUTHOR), Courtioux, Bertrand⁵ (AUTHOR), Azas, Nadine³ (AUTHOR), Rathelot, Pascal^1,2 (AUTHOR), Vanelle, Patrice^1,2 (AUTHOR) nicolas.primas@univ-amu.fr

Source: Molbank. Mar2023, Vol. 2023 Issue 1, pM1573. 7p.

Subject Terms: *AMASTIGOTES, *PYRIDAZINES, *LEISHMANIA donovani, *LEISHMANIA infantum, *CELL survival, *CELL lines

Improving Aqueous Solubility and In Vitro Pharmacokinetic Properties of the 3-Nitroimidazo[1,2- a ]pyridine Antileishmanial Pharmacophore.

Authors: Paoli-Lombardo, Romain¹ (AUTHOR), Primas, Nicolas^1,2 (AUTHOR) nicolas.primas@univ-amu.fr, Bourgeade-Delmas, Sandra³ (AUTHOR) nicolas.primas@univ-amu.fr, Hutter, Sébastien⁴ (AUTHOR), Sournia-Saquet, Alix⁵ (AUTHOR), Boudot, Clotilde⁶ (AUTHOR), Brenot, Emilie⁶ (AUTHOR), Castera-Ducros, Caroline^1,2 (AUTHOR), Corvaisier, Sophie⁷ (AUTHOR), Since, Marc⁷ (AUTHOR), Malzert-Fréon, Aurélie⁷ (AUTHOR), Courtioux, Bertrand⁶ (AUTHOR), Valentin, Alexis³ (AUTHOR), Verhaeghe, Pierre^5,8 (AUTHOR), Azas, Nadine⁴ (AUTHOR), Rathelot, Pascal^1,2 (AUTHOR), Vanelle, Patrice^1,2 (AUTHOR) nicolas.primas@univ-amu.fr

Source: Pharmaceuticals (14248247). Aug2022, Vol. 15 Issue 8, p998-998. 24p.

Subject Terms: *SOLUBILITY, *PYRIDINE, *IMIDAZOPYRIDINES, *STRUCTURE-activity relationships, *PHARMACOKINETICS, *LEISHMANIA donovani, *DRUG solubility

31st Annual GP 2 A Medicinal Chemistry Conference.

Authors: Primas, Nicolas, Castera-Ducros, Caroline, Paoli-Lombardo, Romain, Curti, Christophe, Mathias, Fanny, Rathelot, Pascal, Marchand, Pascal, Vanelle, Patrice

Source: Drugs & Drug Candidates; Mar2024, Vol. 3 Issue 1, p209-243, 35p

Subject Terms: PHARMACEUTICAL chemistry, POSTER presentations, CONFERENCES & conventions, ORAL communication, RESEARCH personnel

Geographic Terms: MARSEILLE (France)

Diethyl (5-Benzyl-2-(4-(N ′-hydroxycarbamimidoyl)phenyl)-5-methyl-4,5-dihydrofuran-3-yl)phosphonate.

Authors: Avendaño Leon, Oscar Leonardo, Curti, Christophe, Santos Urbancg Moncorvo, Fabiana Maia, Kabri, Youssef, Redon, Sébastien, Torres-Santos, Eduardo Caio, Paoli-Lombardo, Romain, Vanelle, Patrice

Source: Molbank; Dec2023, Vol. 2023 Issue 4, pM1736, 6p

Subject Terms: PHOSPHONATES, AMASTIGOTES, NEGLECTED diseases, HYDROXYLAMINE hydrochloride, FREE radicals, FUNCTIONAL groups