276863-95-7Relevant articles and documents
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment
Liu, Wenwen,Wang, Huan,Li, Xiaokang,Xu, Yixiang,Zhang, Jian,Wang, Wei,Gong, Qi,Qiu, Xiaoxia,Zhu, Jin,Mao, Fei,Zhang, Haiyan,Li, Jian
supporting information, p. 3117 - 3125 (2018/05/16)
Depression, a severe mental disease, is greatly difficult to treat and easy to induce other neuropsychiatric symptoms, the most frequent one is cognitive impairment. In this study, a series of novel vilazodone-tacrine hybrids were designed, synthesized and evaluated as multitarget agents against depression with cognitive impairment. Most compounds exhibited good multitarget activities and appropriate blood-brain barrier permeability. Specifically, compounds 1d and 2a exhibited excellent 5-HT1A agonist activities (1d, EC50 = 0.36 ± 0.08 nM; 2a, EC50 = 0.58 ± 0.14 nM) and 5-HT reuptake inhibitory activities (1d, IC50 = 20.42 ± 6.60 nM; 2a, IC50 = 22.10 ± 5.80 nM). In addition, they showed moderate ChE inhibitory activities (1d, AChE IC50 = 1.72 ± 0.217 μM, BuChE IC50 = 0.34 ± 0.03 μM; 2a, AChE IC50 = 2.36 ± 0.34 μM, BuChE IC50 = 0.10 ± 0.01 μM). Good multitarget activities with goodt blood-brain barrier permeability of 1d and 2a make them good lead compounds for the further study of depression with cognitive impairment.
Substituted indole compounds, as well as using method and application thereof
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Paragraph 0144; 0194; 0195; 0196, (2017/08/02)
The invention relates to substituted indole compounds, a using method and application of the substituted indole compounds, as well as a medicine composition including the compounds and application thereof. The compounds or medicine composition can be used for inhibiting reuptake of 5-hydroxytryptamine. The invention further relates to a method for preparing the compounds and the medicine composition, as well as application of the compounds and medicine composition in treatment of central nervous system dysfunction.
Preparation method of substituted indoles compounds
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Paragraph 0015; 0016, (2016/10/07)
The invention belongs to the field of medical technology, and discloses a preparation method of 3-substituted indoles compounds. The preparation method includes using a compound represented by formula (2) as an initial raw material, performing a Friedel-Crafts reaction with 4-chlorobutyryl chloride in the presence of anhydrous titanium tetrachloride catalyst to obtain a compound represented by formula (3), and performing a reaction with paratoluensulfonyl chloride in the presence of an organic solvent and an acid-binding agent to obtain the target compound. The preparation method overcomes the defects of the synthetic method in the prior art, and is suitable for the industrial production. The product has high content, and the purity of the product reaches over 99%.