On July 21, 2022, Chehardoli, Gholamabbas; Gholamhoseini, Pooriya; Ebadi, Ahmad; Ziaei, Maral; Akbarzadeh, Tahmineh; Saeedi, Mina; Mahdavi, Mohammad; Khoshneviszadeh, Mehdi; Najafi, Zahra published an article.COA of Formula: C10H8BrNO2 The title of the article was 6-Methoxy-1-tetralone Derivatives Bearing an N-Arylpyridinium Moiety as Cholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Molecular Docking Study. And the article contained the following:
A novel series of 6-methoxy-1-tetralone derivatives bearing N-aryl pyridinium moiety I (Ar = C6H5, 2-FC6H4, 3-ClC6H4, etc.; n = 1, 2, 3, 4, 5; X = Cl, Br) were designed, synthesized, and evaluated as acetyl and butyrylcholinesterase inhibitors. The designed derivatives inhibited acetylcholinesterase (AChE) with IC50 values of 0.025-23.743μM and butyrylcholinesterase (BChE) with IC50 values of 0.716-20.588μM. The synthesized compounds were divided into two series. Derivatives containing N-benzyl moieties generally were more potent anti-AChE and anti-BChE agents than compounds with N-alkylphthalimide groups. Among them, the compound I (Ar = C6H5; n = 1; X = Br) and compound I (Ar = 3-ClC6H4; n = 1; X = Br) exhibited significant inhibitory activity against AChE and BChE with IC50 values of 0.025 and 0.716μM in comparison to donepezil as a reference drug (0.029 and 0.948μM, resp.). The results of kinetic and mol. modeling studies demonstrated that the synthesized compounds I (Ar = C6H5; n = 1; X = Br) and I (Ar = 3-ClC6H4; n = 1; X = Br) derivatives can act as mixed and dual binding inhibitors, and bind to both CAS and PAS of AChE and BChE enzymes. Among the assessed compounds, the compound I (Ar = C6H5; n = 1; X = Br) indicated significant neuroprotection against H2O2-induced cell death in PC12 cells. So, these findings indicate the therapeutic potential of 6-methoxy-1-tetralone derivatives bearing N-aryl pyridinium moiety derivatives as anti-AD agents. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).COA of Formula: C10H8BrNO2
The Article related to methoxy tetralone aryl pyridinium preparation, mol docking adme inhibitor physicochem property, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.COA of Formula: C10H8BrNO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary