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@ARTICLE{Falkenstein:904311,
      author       = {Falkenstein, Markus and Reiner-Link, David and Zivkovic,
                      Aleksandra and Gering, Ian and Willbold, Dieter and Stark,
                      Holger},
      title        = {{H}istamine {H}3 receptor antagonists with peptidomimetic
                      (keto)piperazine structures to inhibit {A}β
                      oligomerisation},
      journal      = {Bioorganic $\&$ medicinal chemistry},
      volume       = {50},
      issn         = {0968-0896},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier},
      reportid     = {FZJ-2021-05881},
      pages        = {116462 -},
      year         = {2021},
      note         = {Kein Zugriff auf Post-print},
      abstract     = {Alzheimeŕs disease (AD) is the most prominent
                      neurodegenerative disorder with high medical need.
                      Protein-protein-interactions (PPI) interactions have a
                      critical role in AD where β-amyloid structures (Aβ) build
                      toxic oligomers. Design of disease modifying multi target
                      directed ligand (MTDL) has been performed, which disable PPI
                      on the one hand and on the other hand, act as procognitive
                      antagonists at the histamine H3 receptor (H3R). The
                      synthetized compounds are structurally based on
                      peptidomimetic amino acid-like structures mainly as keto,
                      diketo-, or acyl variations of a piperazine moiety connected
                      to an H3R pharmacophore. Most of them showed low nanomolar
                      affinities at H3R and some with promising affinity to
                      Aβ-monomers. The structure–activity relationships (SAR)
                      described offer new possibilities for MTDL with an optimized
                      profile combining symptomatic and potential causal
                      therapeutic approaches in AD.},
      cin          = {IBI-7},
      ddc          = {610},
      cid          = {I:(DE-Juel1)IBI-7-20200312},
      pnm          = {5244 - Information Processing in Neuronal Networks
                      (POF4-524)},
      pid          = {G:(DE-HGF)POF4-5244},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:34695709},
      UT           = {WOS:000710815900002},
      doi          = {10.1016/j.bmc.2021.116462},
      url          = {https://juser.fz-juelich.de/record/904311},
}