Application of polyhydroxy bromo-benzophenone compound and derivatives thereof in treatment and prevention of atherosclerosis

A technology for polyhydroxybromobenzophenone and hydroxybromobenzophenone is applied in the field of medicine, can solve problems such as few applications, and achieve the effects of simple preparation process, easy industrial synthesis and low price

Inactive Publication Date: 2013-06-19
SHANXI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Polyhydroxybrominated benzophenones have protein tyrosine phosphatase 1B (PTP1B) inhibition, α-glucosidase inhibition, antibacterial, antitumor, DPPH free radical scavenging, anti-inflammatory, protein tyrosine kinase (PTKs ) inhibition, biological antifeedant, carbonic sidase inhibition and thrombin inhibition and many other biological activities, but there are few applications in cardiovascular and cerebrovascular diseases such as AS. At present, there are no polyhydroxy brominated benzophenone compounds2,4 Report on the application of ',5'-trihydroxy-5,2'-dibromobenzophenone and its medicinal salts, esters and ethers in the prevention and treatment of AS and other cardiovascular and cerebrovascular diseases

Method used

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  • Application of polyhydroxy bromo-benzophenone compound and derivatives thereof in treatment and prevention of atherosclerosis
  • Application of polyhydroxy bromo-benzophenone compound and derivatives thereof in treatment and prevention of atherosclerosis
  • Application of polyhydroxy bromo-benzophenone compound and derivatives thereof in treatment and prevention of atherosclerosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of medicinal salt of 2,4',5'-trihydroxy-5,2'-dibromobenzophenone

[0031] Weigh 200mg of the sample into a 50mL flask, add 5mL of ethanol, stir and mix, add 20mL of 30% sodium hydroxide solution, stir in a 50°C water bath for 4 hours, add an appropriate amount of absolute ethanol, precipitate a white solid, and filter to obtain its sodium salt , the yield is 21.6%. HRMS (ESI): Calcd. for C 13 h 5 Br 2 Na 3 o 4 : 453.8224; Found: 453.8214.

[0032] .

[0033] Using the same method, 2,4',5'-trihydroxy-5,2'-dibromobenzophenone can react with other inorganic bases and organic bases to obtain its medicinal salts of inorganic bases and organic bases.

Embodiment 2

[0035] 2,4 ’ ,5 ’ -Trihydroxy-5,2 ’ -Preparation of dibromobenzophenone medicinal ester

[0036] Weigh 500mg of the sample into a 100mL flask, add 5g of succinic anhydride in 10mL of anhydrous dichloromethane solution, stir at room temperature, add 1.0g of DCC and 0.5g of DMAP in 20mL of anhydrous dichloromethane solution, stir at room temperature until the reaction of the raw materials is complete, slowly 10 mL of ice water was added to terminate the reaction, the insoluble matter was filtered off, and the organic phase was separated by silica gel chromatography to obtain white crystals with a yield of 45.3%. HRMS (ESI): Calcd. for C 25 h 20 Br 2 o 13 : 687.9336; Found: 687.9326.

[0037] .

[0038] 2,4 ’ ,5 ’ -Trihydroxy-5,2 ’ - Dibromobenzophenone can also react with acetyl chloride, propionyl chloride or acetic anhydride, propionic anhydride to obtain its pharmaceutically acceptable ester.

Embodiment 3

[0040] 2,4 ’ ,5 ’ -Trihydroxy-5,2 ’ -Preparation of dibromobenzophenone medicinal ether

[0041] Weigh 500 mg of sample and dissolve it in 20 mL of acetone, add a little potassium hydroxide, stir, add 10 mL of dimethyl sulfate dropwise, stir at room temperature, until the raw material reacts completely, remove acetone under reduced pressure, and the residue is washed with 10% sodium bicarbonate, After washing with distilled water, the crude product was separated and purified by silica gel chromatography to obtain white crystals with a yield of 37.8%. HRMS (ESI): Calcd. for C 16 h 14 Br 2 o 4 : 429.9227; Found: 429.9217.

[0042] .

[0043] Using the same method, 2,4 ’ ,5 ’ -Trihydroxy-5,2’ -Dibromobenzophenone can also react with diethyl sulfate to obtain its medicinal ether.

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Abstract

The invention discloses application of a polyhydroxy bromo-benzophenone compound and derivatives of the polyhydroxy bromo-benzophenone compound in treatment and prevention of atherosclerosis, and belongs to the technical field of medicines. According to the application of the polyhydroxy bromo-benzophenone compound in the treatment and the prevention of the atherosclerosis, an active ingredient is the polyhydroxy bromo-benzophenone compound 2,4',5'-trihydroxy-5,2'-dibromo-benzophenone, and according to the application of the derivatives of the polyhydroxy bromo-benzophenone compound in the treatment and the prevention of the atherosclerosis, active ingredients are medicinal salt, medicinal ester and medicinal ether of the 2,4',5'-trihydroxy-5,2'-dibromo-benzophenone. Due to the fact that the expression of triglyceride (TG) and low density lipoprotein-cholesterol (LDL-C) in blood serum is reduced, and the expression of inflammatory factors including interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-alpha) and adhesion molecules sICAM-1 in the blood serum is restrained, vascular endothelial injuries are restrained, and vascular endothelia are protected, so that occurrence and development of the atherosclerosis (AS) are restrained, and more broad prospects are opened up for clinical medication.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the pharmaceutical application of polyhydroxy brominated benzophenone compounds in the treatment and prevention of cardiovascular and cerebrovascular diseases, in particular to the application of polyhydroxy brominated benzophenone compounds and their derivatives in the treatment and prevention of cardiovascular and cerebrovascular diseases. Use in prevention of atherosclerosis. Background technique [0002] Atherosclerosis (AS) is a generalized arterial lesion characterized by subintimal lipid deposition, smooth muscle cell and collagen proliferation, and foam cell formation. Thrombosis can lead to ischemic cardiovascular and cerebrovascular diseases and peripheral arterial diseases, which seriously threaten human life and health. [0003] The occurrence and development of AS is the result of the joint action of many factors. There are many theories about its pathogenesis, inclu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61K31/222A61P9/10
Inventor 李青山冯秀娥班树荣
Owner SHANXI MEDICAL UNIV
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