% IMPORTANT: The following is UTF-8 encoded. This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.
@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},
}