Pasieka, Anna published the artcileDiscovery of multifunctional anti-Alzheimer’s agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters, Recommanded Product: (2-Methoxyphenyl)methanamine, the publication is European Journal of Medicinal Chemistry (2021), 113397, database is CAplus and MEDLINE.
Looking for an effective anti-Alzheimer’s agent is very challenging; however, a multifunctional ligand strategy may be a promising solution for the treatment of this complex disease. We herein present the design, synthesis and biol. evaluation of novel hydroxyethylamine derivatives displaying unique, multiple properties that have not been previously reported. The original mechanism of action combines inhibitory activity against disease-modifying targets: β-secretase enzyme (BACE1) and amyloid β (Aβ) aggregation, along with an effect on targets associated with symptom relief – inhibition of butyrylcholinesterase (BuChE) and γ-aminobutyric acid transporters (GATs). Among the obtained mols., compound 36 (I) exhibited the most balanced and broad activity profile (eeAChE IC50 = 2.86μM; eqBuChE IC50 = 60 nM; hBuChE IC50 = 20 nM; hBACE1 IC50 = 5.9μM; inhibition of Aβ aggregation = 57.9% at 10μM; mGAT1 IC50 = 10.96μM; and mGAT2 IC50 = 19.05μM). Moreover, we also identified 31 (II) as the most potent mGAT4 and hGAT3 inhibitor (IC50 = 5.01μM and IC50 = 2.95μM, resp.), with high selectivity over other subtypes. Compounds 36 and 31 represent new anti-Alzheimer agents that can ameliorate cognitive decline and modify the progress of disease.
European Journal of Medicinal Chemistry published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C8H11NO, Recommanded Product: (2-Methoxyphenyl)methanamine.
Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem