Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer’s disease was written by Sang, Zhipei;Wang, Keren;Wang, Huifang;Yu, Lintao;Wang, Huijuan;Ma, Qianwen;Ye, Mengyao;Han, Xue;Liu, Wenmin. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Application of 954-81-4 This article mentions the following:
A series of phthalimide-alkylamine derivs, e.g., I, were synthesized and evaluated as multi-functions inhibitors for the treatment of Alzheimer’s disease (AD). The results showed that compound I could be regarded as a balanced multi-targets active mol. It exhibited potent and balanced inhibitory activities against ChE and MAO-B (huAChE, huBuChE, and huMAO-B with IC50 values of 1.2 婵炴挾鎷? 3.8 婵炴挾鎷?and 2.6 婵炴挾鎷? resp.) with low selectivity. Both kinetic anal. of AChE inhibition and mol. modeling study suggested that I binds simultaneously to the catalytic active site and peripheral anionic site of AChE. Interestingly, compound I abided by Lipinski’s rule of five. Furthermore, our investigation proved that I indicated weak cytotoxicity, and it could cross the blood-brain barrier (BBB) in vitro. The results suggest that compound I, an interesting multi-targeted active mol., offers an attractive starting point for further lead optimization in the drug-discovery process against Alzheimer’s disease. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Application of 954-81-4).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Application of 954-81-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary