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@ARTICLE{Fiorino:141238,
      author       = {Fiorino, Ferdinando and Eiden, Martin and Giese, Armin and
                      Severino, Beatrice and Esposito, Antonella and Groschup,
                      Martin H and Perissutti, Elisa and Magli, Elisa and
                      Incisivo, Giuseppina Maria and Ciano, Antonio and
                      Frecentese, Francesco and Kretzschmar, Hans A and Wagner,
                      Jens and Santagada, Vincenzo and Caliendo, Giuseppe},
      title        = {{S}ynthesis of benzamide derivatives and their evaluation
                      as antiprion agents.},
      journal      = {Bioorganic $\&$ medicinal chemistry},
      volume       = {20},
      number       = {16},
      issn         = {0968-0896},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier},
      reportid     = {DZNE-2020-07560},
      pages        = {5001-5011},
      year         = {2012},
      abstract     = {A new set of
                      5-(2-(pyrrolidin-1-yl)acetamido)-N-butyl-2-(substituted)benzamide
                      and 5-(2-(piperidin-1-yl)acetamido)-N-butyl-2-(substituted)
                      benzamide derivatives were synthesized in which as
                      structural features the 2-(1-pyrrolidinyl)- or
                      2-(1-piperidyl)acetylamino group or a diphenylether moiety
                      are associated to a benzamide scaffold. Their binding
                      affinity for human PrP(C) and inhibition of its conversion
                      into PrP(Sc) were determined in vitro; moreover, the
                      antiprion activity was assayed by inhibition of PrP(Sc)
                      accumulation in scrapie-infected mouse neuroblastoma cells
                      (ScN2a) and scrapie mouse brain (SMB) cells. The results
                      clearly indicate the benzamide derivatives as attractive
                      lead compounds for the development of potential therapeutic
                      agents against prion disease.},
      keywords     = {Animals / Benzamides: chemical synthesis / Benzamides:
                      chemistry / Benzamides: pharmacology / Cell Line /
                      Dose-Response Relationship, Drug / Humans / Mice / Molecular
                      Structure / Prions: antagonists $\&$ inhibitors / Prions:
                      metabolism / Recombinant Proteins: antagonists $\&$
                      inhibitors / Recombinant Proteins: metabolism / Scrapie:
                      drug therapy / Scrapie: metabolism / Structure-Activity
                      Relationship / Benzamides (NLM Chemicals) / Prions (NLM
                      Chemicals) / Recombinant Proteins (NLM Chemicals) /
                      benzamide (NLM Chemicals)},
      cin          = {AG Fuhrmann},
      ddc          = {610},
      cid          = {I:(DE-2719)1011004},
      pnm          = {342 - Disease Mechanisms and Model Systems (POF3-342)},
      pid          = {G:(DE-HGF)POF3-342},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:22795751},
      doi          = {10.1016/j.bmc.2012.06.026},
      url          = {https://pub.dzne.de/record/141238},
}