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Compound towards target of cardiac muscle and preparation

A compound, myocardial technology, applied in the field of medicine, to achieve the effects of enhancing affinity, easy availability of raw materials, and easy control of operation

Inactive Publication Date: 2005-08-31
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some studies have incorporated the non-selective β-receptor blocker allylalol into liposomes, and experiments have shown that this method can increase the distribution of liposomes in the heart, but in β 2 -The lungs with more receptor distribution have more increase, so the liposome is still insufficient as a myocardial targeting drug carrier and needs to be improved

Method used

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  • Compound towards target of cardiac muscle and preparation
  • Compound towards target of cardiac muscle and preparation
  • Compound towards target of cardiac muscle and preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1: Synthesis of Myocardium Targeting Compounds

[0012] Dissolve p-hydroxyphenylpropionic acid in acetone and heat reflux with methyl iodide to obtain methyl p-methoxyphenylpropionate, react it with carbonyl cetyl alcohol to obtain cetyl p-methoxyphenylpropionate, and then mix with Aluminum chloride and mercaptoethanol react at room temperature to obtain cetyl p-hydroxyphenyl propionate, which is refluxed with chloropropylene oxide to obtain (±)-3-[4-(2,3-epoxypropoxy) Phenyl] hexadecyl propionate, and finally reflux reaction with isopropylamine, the product is recrystallized to obtain the target compound (±)-3-{4-[2-hydroxyl-(1-methylethylamino)propoxyl] Cetyl Phenyl}propionate. The synthetic route is as follows:

[0013]

Embodiment 2

[0014] Example 2: Cardiac Targeting of Liposomes Modified by Cardiac Targeting Compounds

[0015] Use a 33mm culture dish to culture neonatal rat cardiomyocytes in vitro. After the cells adhere to the wall and grow into a monolayer, add equimolar fluorescent-labeled common liposomes and 10% modified liposomes of cardiomyocyte targeting compounds, 37°C, 5% CO 2 After culturing in the incubator for 15min, 30min, 1h, 2h, 3h, and 4h, the amount of liposomes taken up by cardiomyocytes surface-connected and endocytosed was measured, and the results are shown in the attached figure 1 shown. The results showed that the liposome formulation modified by the cardiomyocyte targeting compound has remarkable cardiomyocyte targeting.

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Abstract

A cardiac muscle targetable compound (+ / -)-3-{4-[2-hydroxy-(1-methyl ethylamino)propoxy]phenyl} hexadecanol propionate, which is used to modify the surface of liposome, nanoparticles or micro softgel for increaisng the affinity between medicine and cardiac muscle, is prepared from p-hydroxy benzoic acid through esterifying, o-epoxy propylation and isopropylamination.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and specifically it is a myocardial targeting compound and its preparation. Background technique: [0002] Coronary heart disease is one of the main diseases causing human death at present. Due to population aging, obesity, high blood pressure and other reasons, the incidence and mortality of coronary heart disease in my country have shown an obvious upward trend in recent years. It is estimated that coronary heart disease will become the main factor restricting economic development and threatening people's life and health in the 21st century. However, most of the cardiovascular therapeutic drugs (especially protein and polypeptide drugs) affect the therapeutic effect due to the lack of tissue specificity or easy degradation in the body. Therefore, it is an urgent task for medical workers to develop effective myocardial targeting agents. [0003] β-receptor blockers can compete with noradren...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P9/10C07C227/00C07C229/34
Inventor 邓英杰陈研
Owner SHENYANG PHARMA UNIVERSITY
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