Aryl-substituted amide compounds, preparation method thereof, pharmaceutical composition containing same and application thereof
A compound and composition technology, which can be used in the preparation of organic compounds, drug combinations, carboxylic acid amides, etc., can solve the problems of lowering low-density lipoprotein, poor patient tolerance, and large dosage, and achieves the goal of regulating blood lipids, promoting The effect of expulsion
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Embodiment 1
[0111] Example 1: Synthesis of Representative Compounds
[0112] (1) N-(2-(1H-indol-3-yl)ethyl)-2-aminobenzamide (CD1)
[0113] Tryptamine (purchased from Adamas Company, purity>99%) (0.80g, 5mmol) was added in a 50mL round bottom flask, 25mL N, N-dimethylformamide was added, and 2-aminobenzoic acid (0.68g , 5mmol), 1-ethyl-(3-dimethylaminopropyl) carbodiimide (EDCI) hydrochloride (all purchased from Beijing Coupling Technology Co., Ltd., purity> 98%) (0.96g, 5mmol), React overnight at room temperature. Most of the solvent was distilled off under reduced pressure, and after adding 30 mL of water, it was extracted with ethyl acetate and dried over anhydrous sodium sulfate. The ethyl acetate extract was concentrated and eluted through a silica gel column with ethyl acetate:petroleum ether=1:3 to obtain 1.14g of CD1 pure product (yield 82%), white solid, mp159-160°C (literature value 156-157°C). MS(ESIm / z)280.28(M+H) + , HRMS(ESIm / z)[M+H] + Theoretical formula C 17 h 18 N...
Embodiment 2
[0172] Example 2: Activity of Compounds on ABCA1 Up-regulation Screening Model
[0173] ABCA1p-LUC HepG2 cells were obtained from the National Laboratory of New Drugs (Microbiology), Institute of Medical Biotechnology, Chinese Academy of Medical Sciences. For the treatment process of the cells, see, for example, the article Identification of Up-regulators of Human ATP-binding Cassette Transporter Al via High-throughput Screening of Synthetic and Natural Compound Library by Jie Gao et al. Discovery of human ABCA1 up-regulator). J Biomol Screen. 2008, 13(7): 648-656, and Gao Jie's doctoral thesis "Construction and application of a new anti-atherosclerosis drug screening model targeting ABCA1".
[0174] ABCA1-LUC HepG2 cells were added to 5×10 4 Each cell / well was inoculated in a 96-well cell culture plate, and after about 6 hours after the cells adhered to the wall, they were replaced with serum-free RPMI-1640 medium (Hyclone) containing a series of diluted concentrations of th...
Embodiment 3
[0179] Example 3: Activity of Compounds on SR-BI / CLA1 Up-regulator Screening Model
[0180] CLAp-LUC HepG2 was obtained from the National Laboratory of New Drugs (Microorganisms), Institute of Pharmaceutical Biotechnology, Chinese Academy of Medical Sciences. The treatment process of this cell can be referred to for example the article Identification of Novel Human High-Density Lipoprotein Receptor Up-regulators Using a Cell-Based High-Throughput Screening Assay of Yuan Yang et al. In vivo regulator). J Biomol Screen2007, 12(2): 211-219, and Yang Yuan's doctoral thesis "Screening, discovery and related activity research of microorganism-derived high-density lipoprotein receptor upregulators".
[0181] CLAp-LUC HepG2 cells were added to 5×10 4 Each cell / well was inoculated in a 96-well cell culture plate, and after about 6 hours of cell attachment, they were replaced with serum-free MEM-EBSS medium (200 μl / well) containing a series of dilutions of the compound of the present i...
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