@article{fdi:010074883,
  title = {{N}ongenotoxic 3-nitroimidazo[1,2-a]pyridines are {NTR}1 substrates that display potent in vitro antileishmanial activity},
  author = {{F}ersing, {C}. and {B}asmaciyan, {L}. and {B}oudot, {C}. and {P}edron, {J}. and {H}atter, {S}. and {C}ohen, {A}. and {C}astera-{D}ucros, {C}. and {P}rimas, {N}. and {L}aget, {M}. and {C}asanova, {M}. and {B}ourgeade-{D}elmas, {S}andra and {P}iednoel, {M}. and {S}ournia-{S}aquet, {A}. and {M}bou, {V}. {B}. and {C}ourtioux, {B}. and {B}outet-{R}obinet, {E}. and {S}ince, {M}. and {M}ilne, {R}. and {W}yllie, {S}. and {F}airlamb, {A}. {H}. and {V}alentin, {A}. and {R}athelot, {P}. and {V}erhaeghe, {P}. and {V}anelle, {P}. and {A}zas, {N}.},
  editor = {},
  language = {{ENG}},
  abstract = {{T}wenty nine original 3-nitroimidazo[1,2-a]pyridine derivatives, bearing a phenylthio (or benzylthio) moiety at position 8 of the scaffold, were synthesized. {I}n vitro evaluation highlighted compound 5 as an antiparasitic hit molecule displaying low cytotoxicity for the human {H}ep{G}2 cell line ({CC}50 > 100 mu {M}) alongside good antileishmanial activities ({IC}50 = 1-2.1 mu {M}) against {L}. donovani, {L}. infantum, and {L}. major; and good antitrypanosomal activities ({IC}50 = 1.3-2.2 mu {M}) against {T}. brucei brucei and {T}. cruzi, in comparison to several reference drugs such as miltefosine, fexinidazole, eflornithine, and benznidazole ({IC}50 = 0.6 to 13.3 mu {M}). {M}olecule 5, presenting a low reduction potential ({E} degrees = -0.63 {V}), was shown to be selectively bioactivated by the {L}. donovani type 1 nitroreductase ({NTR}1). {I}mportantly, molecule 5 was neither mutagenic (negative {A}mes test), nor genotoxic (negative comet assay), in contrast to many other nitroaromatics. {M}olecule 5 showed poor microsomal stability; however, its main metabolite (sulfoxide) remained both active and nonmutagenic, making 5 a good candidate for further in vivo studies.},
  keywords = {{L}eishmania ssp ; imidazopyridine ; nitroaromatic ; nitroreductases ; {A}mes ; test ; comet assay},
  booktitle = {},
  journal = {{ACS} {M}edicinal {C}hemistry {L}etters},
  volume = {10},
  numero = {1},
  pages = {34--39},
  ISSN = {1948-5875},
  year = {2019},
  DOI = {10.1021/acsmedchemlett.8b00347},
  URL = {https://www.documentation.ird.fr/hor/fdi:010074883},
}