@article{fdi:010053500,
  title = {{A}ryl piperazine and pyrrolidine as antimalarial agents : synthesis and investigation of structure-activity relationships},
  author = {{M}endoza, {A}. and {P}erez-{S}ilanes, {S}. and {Q}uiliano, {M}. and {P}abon, {A}. and {G}aliano, {S}. and {G}onzalez, {G}. and {G}aravito, {G}. and {Z}imic, {M}. and {V}aisberg, {A}. and {A}ldana, {I}. and {M}onge, {A}. and {D}eharo, {E}ric},
  editor = {},
  language = {{ENG}},
  abstract = {{P}iperazine and pyrrolidine derivatives were synthesised and evaluated for their capacity to inhibit the growth of {P}lasmodium falciparum chloroquine-resistant ({FCR}-3) strain in culture. {T}he combined presence of a hydroxyl group, a propane chain and a fluor were shown to be crucial for the antiplasmodial activity. {F}ive compounds of the aryl-alcohol series inhibited 50% of parasite growth at doses <= 10 mu {M}. {T}he most active compound 1-(4-fluoronaphthyl)-3-[4-(4-nitro-2-trifluoromethylphenyl)piperazin-1-y l] propan-1-ol was almost 20-40 times more active on {P}. falciparum ({IC}50: 0.5 mu {M}) than on tumorogenic and non-tumorogenic cells. {I}n vivo it has a very weak effect; inhibiting 35% of parasite growth only, at 10 mg/kg/day against {P}lasmodium berghei infected mice without any impact on survival time. {I}n silico molecular clocking study and molecular electrostatic potential calculation revealed that this compound bound to the active site of {P}lasmodium plasmepsin {II} enzyme.},
  keywords = {{P}iperazine ; {P}yrrolidine ; {A}ntiplasmodial ; {P}lasmodium ; {A}ntimalarial agents ; {D}ocking studies},
  booktitle = {},
  journal = {{E}xperimental {P}arasitology},
  volume = {128},
  numero = {2},
  pages = {97--103},
  ISSN = {0014-4894},
  year = {2011},
  DOI = {10.1016/j.exppara.2011.02.025},
  URL = {https://www.documentation.ird.fr/hor/fdi:010053500},
}