Zang, Yingda; Liu, Ke; Wang, Weiping; Li, Chuangjun; Ma, Jie; Yang, Jingzhi; Chen, Xinyi; Wang, Xiaoliang; Zhang, Dongming published their research in Molecules in 2021. The article was titled 《Claulansine F-donepezil hybrids as anti-Alzheimer’s disease agents with cholinergic, free-radical scavenging, and neuroprotective activities》.Name: 1-(Bromomethyl)-4-chlorobenzene The article contains the following contents:
The multifactorial nature of Alzheimer’s disease (AD) calls for the development of multitarget agents addressing key pathogenic processes. Twenty-six Claulansine F-donepezil hybrids I (X = nothing, CH2, CH2CH2; R1 = OMe, t-Bu; R2 = PhCH2, 2-FC6H4CH2, 4-ClC6H4CH2, etc.) were designed and synthesized as multitarget drugs. Among these compounds, six compounds exhibited excellent acetylcholinesterase (AChE) inhibitory activity (half maximal inhibitory concentration (IC50) 1.63-4.62μM). Moreover, the compound I [X = CH2; R1 = t-Bu; R2 = 2-ClC6H4CH2; (II)] exhibited better neuroprotective effects against OGD/R (oxygen-glucose deprivation/reoxygenation) than lead compound Claulansine F. Furthermore, the compound II could cross the blood-brain barrier in vitro. More importantly, compared to edaravone, the compound II had stronger free-radical scavenging activity. Mol. docking studies revealed that II could interact with the catalytic active site of AChE. All of these outstanding in vitro results indicate the compound II as a leading structure worthy of further investigation.1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7Name: 1-(Bromomethyl)-4-chlorobenzene) was used in this study.
1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7) may be used to synthesize 1-(4-chlorobenzyl)-2-(pyrrolidin-1-yl-methyl)-1H-benzimidazole dihydrochloride.Name: 1-(Bromomethyl)-4-chlorobenzene It can be synthesized by reacting 4-chlorobenzyl alcohol with bromodimethylsulfonium bromide (BDMS) It can also be synthesized by refluxing a mixture of 4-chlorobenzaldehyde, chlorotrimethylsilane, 1,1,3,3-tetramethyldisiloxane and lithium bromide.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics