An antikinetoplastid pharmacomodulation study was conducted at position 6 of the 8-nitroquinolin-2(1H)-one pharmacophore. Fifteen new derivatives were synthesized and evaluated in vitro against L. infantum, T. brucei brucei, and T. cruzi, in parallel with a cytotoxicity assay on the human HepG2 cell line. A potent and selective 6-bromo-substituted antitrypanosomal derivative 12 was revealed, presenting EC 50 values of 12 and 500 nM on T. b. brucei trypomastigotes and T. cruzi amastigotes respectively, in comparison with four reference drugs (30 nM ≤ EC 50 ≤ 13 μM). Moreover, compound 12 was not genotoxic in the comet assay and showed high in vitro microsomal stability (half life >40 min) as well as favorable pharmacokinetic behavior in t...
An antikinetoplastid pharmacomodulation study at position 3 of the recently described hit molecule 3...
To study the antiparasitic 8-nitroquinolin-2(1H)-one pharmacophore, a series of 31 derivatives was s...
An antikinetoplastid pharmacomodulation study was done at position 8 of a previously identified phar...
An antikinetoplastid pharmacomodulation study was conducted at position 6 of the 8-nitroquinolin-2(1...
International audienceAn antikinetoplastid pharmacomodulation study was conducted at position 6 of t...
nitroquinolin-2(1H)-one pharmacophore. Fifteen new derivatives were synthesized and evaluated in vit...
An antikinetoplastid pharmacomodulation study at position 3 of the recently described hit molecule 3...
To study the antiparasitic 8-nitroquinolin-2(1H)-one pharmacophore, a series of 31 derivatives was s...
An antikinetoplastid pharmacomodulation study was done at position 8 of a previously identified phar...
An antikinetoplastid pharmacomodulation study was conducted at position 6 of the 8-nitroquinolin-2(1...
International audienceAn antikinetoplastid pharmacomodulation study was conducted at position 6 of t...
nitroquinolin-2(1H)-one pharmacophore. Fifteen new derivatives were synthesized and evaluated in vit...
An antikinetoplastid pharmacomodulation study at position 3 of the recently described hit molecule 3...
To study the antiparasitic 8-nitroquinolin-2(1H)-one pharmacophore, a series of 31 derivatives was s...
An antikinetoplastid pharmacomodulation study was done at position 8 of a previously identified phar...