Click-designed vanilloid-triazole conjugates as dual inhibitors of AChE and Aβ aggregation

Abstract

Based on their reported neuroprotective properties, vanilloids provide a good starting point for the synthesis of anti-Alzheimer's disease agents.

Design, synthesis and evaluation of imidazo[1,2-a]pyrazin-8(7H)-one derivatives as acetylcholinesterase inhibitors and antioxidants

“…Among the drugs currently approved by the U.S. Food and Drug Administration for the treatment of AD, most are acetylcholinesterase (AChE) inhibitors [20][21][22]. Although inadequate for curing AD, inhibition of AChE remains the most successful strategy and has been shown to be transiently capable of improving memory and cognitive function in AD patients [23,24].…”

Editorial: Experimental and innovative approaches to multi-target treatment of Parkinson's and Alzheimer's diseases - Volume II

“…According to PubMed search, the last year brought 200+ publications related to multi-target or multipurpose treatment of neurodegenerative pathology. Many novel multipotent drugs were introduced, i.e., 4-oxo-N-4-diphenyl butanamides (reversible selective monoamine oxidase B inhibitors with anti-acetylcholinesterase activity) for AD treatment (Jana et al, 2023); benzothiazole derivatives (histamine H3 receptor ligands targeted at acetylcholinesterase, butyrylcholinesterase, and monoamine oxidase B enzymes) for AD therapy (Hafez et al, 2023); vanilloid-triazole conjugates as dual inhibitors of acetylcholinesterase and Aβ aggregation for AD treatment (Elsbaey et al, 2023); N-benzyl piperidine derivatives as potent histone deacetylase and acetylcholinesterase inhibitors for AD therapy (Qin et al, 2023); 5,6-dimethoxyindanone-chalcone-carbamate hybrids as dual inhibitors of acetylcholinesterase and inflammation against AD (Liu et al, 2022); benzimidazole arylhydrazones as antioxidant radical-scavenging agents and MAO-B inhibitors with neuroprotective properties for PD therapy (Anastassova et al, 2022); chalcones as enzyme inhibitors (monoamine oxidase B, catechol-O-methyltransferase, and acetylcholinesterase), inhibitors of α-synuclein aggregation, showing anti-neuroinflammatory activity (inhibition of iNOS or activation of Nrf2 signaling), as well as antagonists of adenosine A1 and/or A2A receptors for PD treatment (Krolicka et al, 2022); resveratrol analogs as dual inhibitors of monoamine oxidase B and carbonic anhydrase VII against neurodegenerative disorders (Carradori et al, 2022).…”