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

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

An antileishmanial structure–activity relationship (SAR) study focused on positions 2 and 8 of the imidazo[1,2-<i>a</i>]pyridine ring was conducted through the synthesis of 22 new derivatives. After being screened on the promatigote and axenic amastigote stages of <i>Leishmania don...

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Bibliographic Details
Main Authors: Romain Paoli-Lombardo, Nicolas Primas, Sandra Bourgeade-Delmas, Sébastien Hutter, Alix Sournia-Saquet, Clotilde Boudot, Emilie Brenot, Caroline Castera-Ducros, Sophie Corvaisier, Marc Since, Aurélie Malzert-Fréon, Bertrand Courtioux, Alexis Valentin, Pierre Verhaeghe, Nadine Azas, Pascal Rathelot, Patrice Vanelle
Format: Article
Language:English
Published: MDPI AG 2022-08-01
Series:Pharmaceuticals
Subjects:
Imidazo[1,2-<i>a</i>]pyridine
nitroaromatic
nitroreductases
<i>Leishmania</i> spp.
structure-activity relationships
thermodynamic solubility
Online Access:https://www.mdpi.com/1424-8247/15/8/998

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https://www.mdpi.com/1424-8247/15/8/998

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