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Sulfur-containing compound with neurological rehabilitation effect and application thereof

A compound and composition technology, applied in the field of medicinal chemistry, to achieve the effects of preventing and treating cranial nerve damage, broadening the scope, and having good therapeutic activity

Active Publication Date: 2021-06-18
THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In summary, although various chemical drugs and natural drugs are in different research stages, there is no currently marketed drug for the prevention or treatment of cranial nerve injury that integrates Fenazinel and JAK kinase inhibitors by means of pharmacophore fusion. drug

Method used

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  • Sulfur-containing compound with neurological rehabilitation effect and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the synthesis of compound 1

[0022] (1) Dissolve compound 2 (0.1mol) in 80mL of trifluoroacetic acid, heat the oil bath to 55°C and react until the reaction is detected by TLC. Acetonitrile: water = 0-100%) to obtain light yellow oil compound 3, yield 45%, HPLC purity 97.3%;

[0023] (2) Dissolve 0.05 mol of compound 3 in 50 mL of acetone, add 0.05 mol of compound 4, 0.1 mol of potassium carbonate and 5.0 mmol of potassium iodide at room temperature, raise the temperature to reflux until the reaction is detected by TLC, cool the reaction solution to room temperature, pump After filtration, the filtrate was concentrated under reduced pressure and recrystallized from methanol to obtain white crystal compound 1 with a yield of 86% and a purity of 99.6% by HPLC.

[0024] Molecular formula: C 22 h 25 N 3 o 2 S; ESI-MS: 396.61 [M+H] +

[0025] 1 H NMR (400MHz, CDCl 3 ): δ2.23-2.60 (m, 4H), 2.69-2.95 (m, 3H), 3.26 (s, 2H), 3.61 (m, 3H), 4.32 (s, 2H), 7....

Embodiment 2

[0026] Example 2: Pharmacodynamic screening research on glutamate-induced neuronal excitatory effect of compound represented by formula 1

[0027] Observe glutamate-induced neuronal damage and the possible neuroprotective effect of the target test compound on the cell model, and compare with positive test products.

[0028] 1. Animals and materials

[0029] Compound 1, self-made, HPLC purity 99.0%; DW-2000 Brain Stereotaxic Instrument (Chengdu Taimeng Software Co., Ltd.); positive control substance Fenazinel dihydrochloride, purchased from Shanghai Pharmaceutical Industry Research Institute; sterile PBS, purchased from Shanghai Yuanmu Biotechnology Ltd.; SH-SY5Y human neuroblastoma cell carcinoma cells were purchased from Shanghai Enzyme Biotechnology Co., Ltd.

[0030] 2. Experimental method

[0031] 2.1 Cell culture

[0032] SY5Y cells were cultured in DMEM medium containing 10% fetal bovine serum at 37°C, 5% CO2, and the medium was changed every 3 days. Trypsinization o...

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Abstract

The invention relates to a sulfur-containing compound with a neurological rehabilitation effect, which has good treatment and rehabilitation effects on cerebral nerve injury diseases such as cerebral apoplexy and the like, and shows substantive scientific progress and outstanding beneficial effects compared with existing medicines.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a sulfur-containing compound with neurorestorative effect, and also relates to a preparation method, pharmaceutical composition and use of the compound. Background technique [0002] Intracerebral hemorrhage (ICH) is one of the main diseases of acute cerebrovascular disease and a common disease in neurology and surgery. It has the characteristics of critical onset, high disability rate and high mortality rate. It occurs within a few hours after the hemorrhage, and the hematoma spreads very quickly after the intracranial hematoma appears. If it is not treated in time, cerebral edema may occur and neurological function will be damaged. Neurological function further declines in most cases due to secondary injury. [0003] The current drugs for the treatment of cerebral nerve damage caused by stroke aim to block the neuronal necrosis caused by ischemia, prolong the time of tolerab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D513/08A61P25/00A61K31/4995
CPCA61P25/00C07D513/08
Inventor 李维平黄贤键谭回
Owner THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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