Nongenotoxic 3-Nitroimidazo[1,2-a]pyridines Are NTR1 Substrates That Display Potent in Vitro Antileishmanial Activity.

ABSTRACT: Twenty nine original 3-nitroimidazo[1,2-a]pyridine derivatives, bearing a phenylthio (or benzylthio) moiety at position 8 of the scaffold, were synthesized. In vitro evaluation highlighted compound 5 as an antiparasitic hit molecule displaying low cytotoxicity for the human HepG2 cell line (CC₅₀ > 100 μM) alongside good antileishmanial activities (IC₅₀ = 1-2.1 μM) against L. donovani, L. infantum, and L. major; and good antitrypanosomal activities (IC₅₀ = 1.3-2.2 μM) against T. brucei brucei and T. cruzi, in comparison to several reference drugs such as miltefosine, fexinidazole, eflornithine, and benznidazole (IC₅₀ = 0.6 to 13.3 μM). Molecule 5, presenting a low reduction potential (

SUBMITTER: Fersing C 

PROVIDER: S-EPMC6331159 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature