6-Methoxy-1-tetralone Derivatives Bearing an N-Arylpyridinium Moiety as Cholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Molecular Docking Study was written by Chehardoli, Gholamabbas;Gholamhoseini, Pooriya;Ebadi, Ahmad;Ziaei, Maral;Akbarzadeh, Tahmineh;Saeedi, Mina;Mahdavi, Mohammad;Khoshneviszadeh, Mehdi;Najafi, Zahra. And the article was included in ChemistrySelect in 2022.Product Details of 954-81-4 This article mentions 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 0.025-23.743娓璏 and butyrylcholinesterase (BChE) with IC50 values of 0.716-20.588娓璏. 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 0.716娓璏 in comparison to donepezil as a reference drug (0.029 and 0.948娓璏, 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. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Product Details of 954-81-4).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Product Details of 954-81-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary