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000904311 1001_ $$00000-0001-9785-2100$$aFalkenstein, Markus$$b0
000904311 245__ $$aHistamine H3 receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation
000904311 260__ $$aAmsterdam [u.a.]$$bElsevier$$c2021
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000904311 520__ $$aAlzheimeŕs 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.
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000904311 7001_ $$00000-0003-1514-2215$$aReiner-Link, David$$b1
000904311 7001_ $$00000-0001-5034-7916$$aZivkovic, Aleksandra$$b2
000904311 7001_ $$0P:(DE-Juel1)171922$$aGering, Ian$$b3
000904311 7001_ $$0P:(DE-Juel1)132029$$aWillbold, Dieter$$b4$$ufzj
000904311 7001_ $$00000-0003-3336-1710$$aStark, Holger$$b5$$eCorresponding author
000904311 773__ $$0PERI:(DE-600)1501507-5$$a10.1016/j.bmc.2021.116462$$gVol. 50, p. 116462 -$$p116462 -$$tBioorganic & medicinal chemistry$$v50$$x0968-0896$$y2021
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