54244-58-5Relevant articles and documents
Histamine H3 receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation
Falkenstein, Markus,Reiner-Link, David,Zivkovic, Aleksandra,Gering, Ian,Willbold, Dieter,Stark, Holger
, (2021/10/29)
Alzheime?s 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.
β-strand mimicking macrocyclic amino acids: Templates for protease inhibitors with antiviral activity
Glenn, Matthew P.,Pattenden, Leonard K.,Reid, Robert C.,Tyssen, David P.,Tyndall, Joel D. A.,Birch, Christopher J.,Fairlie, David P.
, p. 371 - 381 (2007/10/03)
New amino acids are reported in which component macrocycles are constrained to mimic tripeptides locked in a β-strand conformation. The novel amino acids involve macrocycles functionalized with both an N- and a C-terminus enabling addition of appendages a
IMMUNOACTIVE PEPTIDES. I. SYNTHESIS OF ACTIVE FRAGMENTS OF SOME PEPTIDE HORMONES ON THE THYMUS
Martynov, V. F.,Anokhina, V. V.,Belokrylov, G. A.,Leont'eva, L. I.,Sorochinskaya, E. I.
, p. 2122 - 2128 (2007/10/02)
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