Onder, Ferah Comert; Sahin, Kader; Senturk, Murat; Durdagi, Serdar; Ay, Mehmet published an article in 2022. The article was titled 《Identifying highly effective coumarin-based novel cholinesterase inhibitors by in silico and in vitro studies》, and you may find the article in Journal of Molecular Graphics & Modelling.Recommanded Product: 1-Methylpiperazine The information in the text is summarized as follows:
Inhibition of high cholinesterase levels including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), is one of the most important strategies for the treatment of Alzheime′s disease (AD). Clin. limited drugs are used in the treatment of AD, so there is a need to find new effective inhibitors today. Therefore, in this study, synthesized six coumarin carboxamides (A1, A2, B1-B4) were evaluated against AChE and BChE by combined in silico and in vitro studies. The in vitro assessment of studied compounds revealed that A1, A2, B3, and B4 showed highest inhibition potential against AChE and BChE. As demonstrated with our structure activity relationship (SAR) study, the promising inhibition result of AChE at nanomolar concentrations was obtained with heterocyclic amines including pyrrolidine and N-Me piperazine moieties for tertiary amide substituted coumarin compounds B3 and B4, displaying KI values of 9.78 nM and 8.07 nM, resp. Thus, compounds B3 and B4 had around 5.7- and 6.9-fold more potency compared to the reference mol., neostigmine. Moreover, coumarin-3-carboxamide derivative A1 bearing benzylmorpholine moiety on coumarin scaffold at position 3 displayed stronger inhibition potential against BChE. Furthermore, in order to better understand their mol. mechanisms in these targets, we conducted mol. docking and MD simulations. Our promising preclin. results show that the lead compounds A1, A2, B3 and B4 have high potential as effective inhibitors for the treatment of AD. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics