20714-90-3Relevant articles and documents
Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
Yang, Jie,Yun, Yinling,Miao, Yuhang,Sun, Jie,Wang, Xiaojing
, p. 805 - 814 (2020/03/23)
Multi-target drugs can better address the cascade of events involved in oxidative stress and the reduction in cholinergic transmission that occur in Alzheimer’s disease than cholinesterase inhibitors alone. We synthesised a series of 3-arylbenzofuranone derivatives and evaluated their antioxidant activity, cholinesterase inhibitory activity, and monoamine oxidase inhibitory activity. 3-Arylbenzofuranone compounds exhibit good antioxidant activity as well as selective acetylcholinesterase inhibitory activity. The IC50 value of anti-acetylcholinesterase inhibition of Compound 20 (0.089 ± 0.01 μM) is similar to the positive drug donepezil (0.059 ± 0.003 μM). According to the experimental results, Compounds 7, 13 show a certain effect in the in?vitro evaluation performed and have the potential as drug candidates for the treatment of Alzheimer’s disease.
Structure-activity relationships study of neolamellarin A and its analogues as hypoxia inducible factor-1 (HIF-1) inhibitors
Li, Guangzhe,Dong, Huijuan,Ma, Yao,Shao, Kun,Li, Yueqing,Wu, Xiaodan,Wang, Shisheng,Shao,Zhao, Weijie
supporting information, p. 2327 - 2331 (2019/07/09)
The novel marine pyrrole alkaloid neolamellarin A derived from sponge has been shown to inhibit hypoxia-induced HIF-1 activity. In this work, we designed and synthesized neolamellarin A and its series of derivatives by a convergent synthetic strategy. The HIF-1 inhibitory activity and cytotoxicity of these compounds were evaluated in Hela cells by dual-luciferase reporter gene assay and MTT assay, respectively. The results showed that neolamellarin A 1 (IC50 = 10.8 ± 1.0 μM) and derivative 2b (IC50 = 11.9 ± 3.6 μM) had the best HIF-1 inhibitory activity and low cytotoxicity. Our SAR research focused on the effects of key regions aliphatic carbon chain length, aromatic ring substituents and C-7 substituent on biological activity, providing a basis for the subsequent research on the development of novel pyrrole alkaloids as HIF-1 inhibitors and design of small molecule probes for target protein identification.
Method for preparing phenylethanolamine compound intermediate
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Paragraph 0070, (2018/05/07)
The invention discloses a method for preparing a phenylethanolamine compound intermediate. The method comprises the following steps: (1) carrying out a nitrifying reaction on 1-methyl-3-phenylpropylamine and a nitrifying reagent to obtain a 4-(4-nitrophenyl)-butan-2-amine and 4-(2-nitrophenyl)-butan-2-amine mixture; and (2) reacting the mixture obtained in step (1) with a compound of formula III,and separating the obtained reaction product to obtain the phenylethanolamine compound intermediate of formula I. The method for preparing the phenylethanolamine compound intermediate has the advantages of simplicity in operation, short route and few steps; and an o-nitro impurities generated in the nitrifying reaction can be easily removed after being reacted without separation and becoming corresponding amides, so the reaction yield and the product purity are high, and the industrial production of the product is facilitated.
