BIP! Finder - 8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases

2018 • 8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases

Authors: Cyril Fersing; Clotilde Boudot; Julien Pedron; Sébastien Hutter; Nicolas Primas; Caroline Castera-Ducros; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Alain Moreau; Anita Cohen; Jean-Luc Stigliani; Geneviève Pratviel; Maxime D. Crozet; Susan Wyllie; Alan Fairlamb; Alexis Valentin; Pascal Rathelot; Nadine Azas; Bertrand Courtioux; Pierre Verhaeghe; Patrice Vanelle

Venue: European Journal of Medicinal Chemistry

Type: Publication

Abstract: Based on a previously identified antileishmanial 6,8-dibromo-3-nitroimidazo[1,2-a]pyridine derivative, a Suzuki-Miyaura coupling reaction at position 8 of the scaffold was studied and optimized from a 8-bromo-6-chloro-3-nitroimidazo[1,2-a]pyridine substrate. Twenty-one original derivatives were prepared, screened in vitro for activity against L. infantum axenic amastigotes and T. brucei brucei trypomastigotes and evaluated for their cytotoxicity on the HepG2 human cell line. Thus, 7 antileishmanial hit compounds were identified, displaying IC50... (read more)

Impact:

1.47191646E-8 3.3689096E-9 19 11

/ Attention: 0 19

Topics: Stereochemistry

DOI: 10.1016/j.ejmech.2018.07.064

External links: Crossref OpenAIRE

Related works: Dataset 2

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