On June 10, 2021, Yao, Hong; Uras, Giuseppe; Zhang, Pengfei; Xu, Shengtao; Yin, Ying; Liu, Jie; Qin, Shuai; Li, Xinuo; Allen, Stephanie; Bai, Renren; Gong, Qi; Zhang, Haiyan; Zhu, Zheying; Xu, Jinyi published an article.Formula: C7H6ClNO2 The title of the article was Discovery of Novel Tacrine-Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer’s Disease. And the article contained the following:
Based on a multitarget strategy, a series of novel tacrine-pyrimidone hybrids were identified for the potential treatment of Alzheimer’s disease (AD). Biol. evaluation results demonstrated that these hybrids exhibited significant inhibitory activities toward acetylcholinesterase (AChE) and glycogen synthase kinase 3 (GSK-3). The optimal compound 27g (I) possessed excellent dual AChE/GSK-3 inhibition both in terms of potency and equilibrium (AChE: IC50 = 51.1 nM; GSK-3β: IC50 = 89.3 nM) and displayed significant amelioration on cognitive deficits in scopolamine-induced amnesia mice and efficient reduction against phosphorylation of tau protein on Ser-199 and Ser-396 sites in glyceraldehyde (GA)-stimulated differentiated SH-SY5Y cells. Furthermore, compound 27g exhibited eligible pharmacokinetic properties, good kinase selectivity, and moderate neuroprotection against GA-induced reduction in cell viability and neurite damage in SH-SY5Y-derived neurons. The multifunctional profiles of compound 27g suggest that it deserves further investigation as a promising lead for the prospective treatment of AD. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Formula: C7H6ClNO2
The Article related to tacrine pyrimidone hybrid ache gsk3 inhibitor alzheimer disease, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Formula: C7H6ClNO2
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