@article{fdi:010068947,
  title = {{E}xploring the scope of new arylamino alcohol derivatives : synthesis, antimalarial evaluation, toxicological studies, and target exploration},
  author = {{Q}uiliano, {M}. and {M}endoza, {A}. and {F}ong, {K}. {Y}. and {P}abon, {A}. and {G}oldfarb, {N}. {E}. and {F}abing, {I}. and {V}ettorazzi, {A}. and de {C}erain, {A}. {L}. and {D}unn, {B}. {M}. and {G}aravito, {G}. and {W}right, {D}. {W}. and {D}eharo, {E}ric and {P}erez-{S}ilanes, {S}. and {A}ldana, {I}. and {G}aliano, {S}.},
  editor = {},
  language = {{ENG}},
  abstract = {{S}ynthesis of new 1-aryl-3-substituted propanol derivatives followed by structure-activity relationship, in silico drug-likeness, cytotoxicity, genotoxicity, in silico metabolism, in silico pharmacophore modeling, and in vivo studies led to the identification of compounds 22 and 23 with significant in vitro anti-plasmodial activity against drug sensitive ({D}6 {IC}50 <= 0.19 mu {M}) and multidrug resistant ({FCR}-3 {IC}50 <= 0.40 mu {M} and {C}235 {IC}50 <= 0.28 mu {M}) strains of {P}lasmodium falciparum. {A}dequate selectivity index and absence of genotoxicity was also observed. {N}otably, compound 22 displays excellent parasitemia reduction (98 +/- 1%), and complete cure with all treated mice surviving through the entire period with no signs of toxicity. {O}ne important factor is the agreement between in vitro potency and in vivo studies. {T}arget exploration was performed; this chemotype series exhibits an alternative antimalarial mechanism.},
  keywords = {{A}ntimalarial ; {A}ntiplasmodial ; {A}rylamino alcohol ; {P}lasmepsin {II} enzyme ; {H}emozoin inhibition ; {M}annich reaction},
  booktitle = {},
  journal = {{I}nternational {J}ournal for {P}arasitology-{D}rugs and {D}rug {R}esistance},
  volume = {6},
  numero = {3},
  pages = {184--198},
  ISSN = {2211-3207},
  year = {2016},
  DOI = {10.1016/j.ijpddr.2016.09.004},
  URL = {https://www.documentation.ird.fr/hor/fdi:010068947},
}