Application of magnolol derivatives in preparing drugs for treating central nervous system diseases

A technology of phenol derivatives and central nervous system, applied in the field of phenolic compound magnolol derivatives or their pharmaceutically acceptable salts and their pharmaceutical compositions, can solve the problem of no biological activity and no reports of magnolol derivatives And other issues

Inactive Publication Date: 2018-12-14
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Magnolol derivatives (1-7) are obtained for the first time by chemical synthesis using magnolol as a raw material. In the prior art, there is no report about the magnolol derivatives 1-7, and there is no report about its biological activity. to report

Method used

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  • Application of magnolol derivatives in preparing drugs for treating central nervous system diseases
  • Application of magnolol derivatives in preparing drugs for treating central nervous system diseases
  • Application of magnolol derivatives in preparing drugs for treating central nervous system diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 1. Preparation of compounds 1-3,6:

[0024] In a reaction vial, dissolve 0.3 mM magnolol in dry dichloromethane and add the substrate (1.5 equiv), which is 3-chloropropionic acid. Dehydrating agent DCC and catalyst DMAP (0.05 equiv), stirred and reacted at room temperature for 4 hours, after the reaction of the raw materials was detected by TLC, the reaction solution was filtered to remove the precipitate, and the filtrate was separated and purified by silica gel column chromatography to obtain compound 1; In, 0.3mM magnolol was dissolved in dry dichloromethane, and the substrate (1.5equiv) was added, the substrate was 4-chlorobutyric acid. Dehydrating agent DCC and catalyst DMAP (0.05 equiv), stirred and reacted at room temperature for 4 hours, after the reaction of the raw materials was detected by TLC, the reaction solution was filtered to remove the precipitate, and the filtrate was separated and purified by silica gel column chromatography to obtain compound 2; In...

Embodiment 2

[0044] The effect of compounds 1-7 on melatonin receptor MT 1 and MT 2 Agonistic activity of the receptor.

[0045] 1 Materials and methods

[0046] 1.1 Materials:

[0047] melatonin receptor MT 1 and MT 2 The cell lines used for agonistic activity screening correspond to human kidney epithelial cells HEK293-MT 1 and HEK293-MT 2 ; Cell culture medium (Dulbecco's Modified Eagle Medium, DMEM) containing 10% fetal bovine serum; No-wash calcium flow kit.

[0048] 1.2 Instrument: CO 2 Constant temperature incubator Thermo Forma 3310 (USA); Inverted biological microscope XD-101 (Nanjing); Flexstation 3Benchtop Multi-Mode Microplate Reader (Molecular Devices, Sunnyvale, California, USA).

[0049] 1.3 Experimental process

[0050] Coat the 96-well black-walled transparent-bottom cell culture plate with the substrate BD Matrigel, put it in a constant temperature incubator at 37°C for 1 hour, absorb the supernatant, and dilute it with 4×10 4 Density per well, the corresponding H...

preparation Embodiment

[0061] 1. Compound 1-7 was prepared according to the method of Example 1. After dissolving with a small amount of DMSO, water for injection was added as usual, finely filtered, potted and sterilized to make an injection.

[0062] 2. Compound 1-7 was prepared according to the method of Example 1. After dissolving with a small amount of DMSO, it was dissolved in sterile water for injection, stirred to dissolve, filtered with a sterile suction filter funnel, and then sterile finely filtered. Packed in ampoules, freeze-dried at low temperature and sealed aseptically to obtain powder injection.

[0063] 3. According to the method of Example 1, the compound 1-7 was firstly prepared, and the excipient was added according to the weight ratio of the compound 1-7 to the excipient at a ratio of 9:1 to make a powder.

[0064] 4. According to the method of Example 1, the compound 1-7 was firstly prepared, and the excipient was added according to the weight ratio of the compound 1-7 to the ...

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Abstract

The invention belongs to the technical field of drugs and provides magnolol derivatives (1-7) as shown in a structural formula (I) or a pharmaceutical composition and application of the magnolol derivatives or the pharmaceutical composition in preparing a melatonin receptor agonist as well as application thereof in preparing drugs for treating or preventing melatonin receptor related central nervous system diseases.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to derivatives (1-7) of phenolic compound magnolol or its pharmaceutically acceptable salts and pharmaceutical compositions thereof, which are used as melatonin receptor agonists, and are used in the preparation of treatments or preventions related to melatonin Drug application in the central nervous system diseases related to hormone receptors. Background technique [0002] Melatonin (N-acetyl-5-methoxytryptamine, Melatonin) is an amine hormone mainly produced by the pineal gland in the human body. It was first isolated from bovine pineal tissue by Lerner et al. in 1958. The production of melatonin is mainly through the conversion of L-tryptophan into 5-hydroxytryptamine in pineal cells, and then generates N-acetyl 5-hydroxytryptamine under the action of N-acetyltransferase (AA-NAT), and finally in 5-hydroxytryptamine. Melatonin is produced by the enzyme oxindoleox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/63C07C69/618C07H15/203C07H1/08A61K31/216A61K31/222A61K31/7034A61P25/00
CPCA61K31/7034A61P25/00C07C69/618C07C69/63C07H1/08C07H15/203
Inventor 陈纪军杨通华耿长安颜得秀马云保黄晓燕张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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