54120-66-0Relevant academic research and scientific papers
MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF
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, (2021/01/23)
The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
A Hg(OTf)2-Catalyzed Enolate Umpolung Reaction Enables the Synthesis of Coumaran-3-ones and Indolin-3-ones
Dai, Ning,Hu, Weican,Qian, Guoying,Rong, Zhouting
, p. 3286 - 3290 (2020/04/21)
The potential of mercury catalysis has been extended to the arena of enolate umpolung reactions for the first time by the generation of enolonium species via Hg(OTf)2-catalyzed N-oxide addition to alkynes. The enolonium species formed can undergo intramolecular nucleophilic attack by hydroxyl or amino groups, leading to the synthesis of various coumaran-3-ones and indolin-3-ones.
Catalytic synthesis method of 3-benzofuranone compound
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Paragraph 0018; 0019, (2020/05/14)
The invention discloses a catalytic synthesis method of a 3-benzofuranone compound. The catalytic synthesis method comprises the following steps: dissolving a 2-acetenyl phenol derivative into a solvent dichloromethane at normal temperature and normal pressure according to a molar volume ratio of the 2-acetenyl phenol derivative to the dichloromethane of 1:5mmol/mL, so as to obtain a dichloromethane solution of the 2-acetenyl phenol derivative; then adding mercury trifluoromethanesulfonate and pyridine-N-oxide into a dichloromethane solution of the 2-ethynylphenol derivative, wherein the molaramounts of mercury trifluoromethanesulfonate and pyridine-N-oxide are respectively 5% and 120% of the molar amount of the 2-ethynylphenol derivative; and then performing stirring for 1 hour at room temperature, and performing reacting to generate the 3-benzofuranone compound. The market price of the catalyst mercury trifluoromethanesulfonate used in the catalytic synthesis method is lower than 30yuan/g, the cost is low, the operation is simple, the reaction time is short, the reaction conditions are mild, the reaction yield is high, and the yield can reach 91.0-96.0%.
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet β-cells from apoptosis
Wang, Sheng,Xu, Lei,Lu, Yu-Ting,Liu, Yu-Fei,Han, Bing,Liu, Ting,Tang, Jie,Li, Jia,Wu, Jiangping,Li, Jing-Ya,Yu, Li-Fang,Yang, Fan
, p. 195 - 208 (2017/03/02)
Death-associated protein kinase-related apoptosis-inducing kinase-2 (DRAK2) is a serine/threonine kinase that plays a key role in a wide variety of cell death signaling pathways. Inhibition of DRAK2 was found to efficiently protect islet β-cells from apoptosis and hence DRAK2 inhibitors represent a promising therapeutic strategy for the treatment of diabetes. Only very few chemical entities targeting DRAK2 are currently known. We carried out a high throughput screening and identified compound 4 as a moderate DRAK2 inhibitor with an IC50value of 3.15?μM. Subsequent SAR studies of hit compound 4 led to the development of novel benzofuran-3(2H)-one series of DRAK2 inhibitors with improved potency and favorable selectivity profiles against 26 selected kinases. Importantly, most potent compounds 40 (IC50?=?0.33?μM) and 41 (IC50?=?0.25?μM) were found to protect islet β-cells from apoptosis in dose-dependent manners. These data support the notion that small molecule inhibitors of DRAK2 represents a promising strategy for the treatment of diabetes.
Practical, modular, and general synthesis of 3-coumaranones through gold-catalyzed intermolecular alkyne oxidation strategy
Shu, Chao,Liu, Rongfu,Liu, Shuang,Li, Jian-Qiao,Yu, Yong-Fei,He, Qiao,Lu, Xin,Ye, Long-Wu
supporting information, p. 91 - 95 (2015/02/19)
A gold-catalyzed intermolecular alkyne oxidation for the preparation of 3-coumaranones has been developed. Using 8-isopropylquinoline N-oxides as oxidants, the reactions of o-ethynylanisoles afford versatile 3-coumaranones in moderate to good isolated yields. The synthetic utility of this chemistry is also indicated by the synthesis of the natural product sulfuretin.
Synthesis, antibacterial activity, and quantitative structure-activity relationships of new (Z)-2-(nitroimidazolylmethylene)-3(2 H)-benzofuranone derivatives
Hadj-esfandiari, Narges,Navidpour, Latifeh,Shadnia, Hooman,Amini, Mohsen,Samadi, Nasrin,Faramarzi, Mohammad Ali,Shafiee, Abbas
, p. 6354 - 6363 (2008/09/21)
A new series of (Z)-2-(1-methyl-5-nitroimidazole-2-ylmethylene)-3(2 H)-benzofuranones (11a-p) and (Z)-2-(1-methyl-4-nitroimidazole-5-ylmethylene)-3(2 H)-benzofuranones (12a-m) were synthesized and assayed for their antibacterial activity against Gram-positive and Gram-negative bacteria. Most of the 5-nitroimidazole analogues (11a-p) showed a remarkable inhibition of a wide spectrum of Gram-positive bacteria (Staphylococcus aureus, Streptococcus epidermidis, MRSA, and Bacillus subtilis) and Gram-negative Klebsiella pneumoniae, whereas 4-nitroimidazole analogues (12a-m) were not effective against selected bacteria. The quantitative structure-activity relationship investigations were applied to find out the correlation between the experimentally evaluated activities with various parameters of the compounds studied. The QSAR models built in this work had reasonable predictive power and could be explained by the observed trends in activities.
Synthesis of 3-(3-Benzofuranyl)coumarins
Deshpande, A.R.,Paradkar, M.V.
, p. 809 - 816 (2007/10/02)
The paper describes the synthesis of a new ring system 3-(3-benzofuranyl)coumarins.
