Application of [1'-(7''-chlorine-quinoline-4''-base) diethylenediamine-4'-base]-3-propionic acid in preparing anti-malarials

An anti-malarial and drug technology, applied in the direction of drug delivery, anti-infective drugs, drug combination, etc., can solve the problems of chemical properties, biological activities and uses of compounds without research, molecular structure is difficult to infer biological activities and uses, etc.

Inactive Publication Date: 2010-04-14
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The article "Piperaquine bioanalysis, drug metabolism and pharmacokinetics" made a more in-depth study on the pharmacodynamics and drug metabolism of piperaquine in the human body, and found that piperaquine has 5 main metabolites after being absorbed and utilized by the human body, one of which is It is [1'-(7"-chloro-quinolin-4"-yl) piperazin-4'-yl]-3-propionic acid, its structure is shown in formula I, but the paper does not have chemical information on this compound It is difficult to deduce its biological activity and use only based on the molecular structure

Method used

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  • Application of [1'-(7''-chlorine-quinoline-4''-base) diethylenediamine-4'-base]-3-propionic acid in preparing anti-malarials
  • Application of [1'-(7''-chlorine-quinoline-4''-base) diethylenediamine-4'-base]-3-propionic acid in preparing anti-malarials
  • Application of [1'-(7''-chlorine-quinoline-4''-base) diethylenediamine-4'-base]-3-propionic acid in preparing anti-malarials

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0064] One, the preparation of [1'-(7"-chloro-quinoline-4"-yl) piperazin-4'-yl]-3-propionic acid:

[0065] 1. Forty-five healthy subjects, aged 20-30 years and weighing 45-75kg, who did not take any drugs within one week before the experiment, took Artekin tablets for four consecutive times at 0, 6, 24 and 32 hours, two tablets each time, and collected About 155L of urine was collected for 5 days after the medicine, which was used for separation and analysis.

[0066] 2. Separation and purification of metabolite M1 in human urine samples

[0067] (1) Concentrate the collected urine to 4L, then extract it with 3 times the volume of a mixed solvent of dichloromethane, ether and isopropanol at a volume ratio of 15:10:1, and take the water layer;

[0068] (2) Concentrate the water layer to 1500mL, pass through the AB8 macroporous resin, elute with water first, then use 5%-30% ethanol gradient elution, collect and combine the eluate of 10-30% ethanol;

[0069] (3) Concentrate 5ml...

example 2

[0081] Example 2 Injection

[0082] Take 0.3 g of the compound obtained in Example 1, add water to make a 30% (w / w) liquid medicine, filter it through a 0.45 μm microporous membrane, put it in a 5 mL vial, and freeze-dry it: pre-freeze at -30 ° C for 3 hr , the vacuum degree reached 1232mTorr; the first stage was heated to 5°C and maintained for 10hr; the second stage was heated to 35°C and maintained for 10hr to obtain the lyophilized powder of the compound.

[0083] The freeze-dried powder can be dissolved within 20 seconds after adding water for injection (0.9% NaCl). When in use, use water for injection (0.9% NaCl) to prepare 3 mg / mL injection.

example 3

[0085] Prescription: Example 1 obtained compound 40g mannitol 48g

[0086] Microcrystalline Cellulose 32g Low Substituted Hydroxypropyl Cellulose (L-HPC) 8g

[0087] Micronized silica gel 0.4g Magnesium stearate 0.4g

[0088] A total of 200 tablets were made.

[0089] Preparation method: take microcrystalline cellulose and dry it at 80°C for 4 hours, mix it with L-HPC, mannitol, and the compound obtained in Example 1 in sequence, add magnesium stearate, and micropowder silica gel to mix, and directly compress tablets with an appropriate pressure to make a total of 200 Tablets, each containing 200mg of [1'-(7"-chloro-quinolin-4"-yl)piperazin-4'-yl]-3-propionic acid.

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Abstract

The invention relates to the pharmaceutical use of (1'-(7''-chlorine-quinoline-4''-radix) piperazine-4'-radix)-3-monoprop. The (1'-(7''-chlorine-quinoline-4''-radix) piperazine-4'-radix)-3-monoprop isa product of the metabolism of human body, which can inhibit the growth of malaria parasites and the fission of the schizont thereof, and can be used for the preparation of anti-malarial drugs.

Description

technical field [0001] The invention relates to the field of organic chemistry, in particular to a compound containing a quinoline ring. Background technique [0002] Quinoline (quinoline) is a compound of pyridine and benzene in parallel, the molecular formula is C 9 h 7 N, mainly used to prepare dyes or as pharmaceutical intermediates, and its derivatives are various, including piperaquine and its phosphate, chloroquine, quinine, mefloquine and primary ammonia Primaquine is a commonly used drug against malaria. [0003] Piperaquine and its phosphate are currently better antimalarial drugs, which have a radical effect on chloroquine-resistant falciparum malaria, but the effect is slow. The article "Piperaquine bioanalysis, drug metabolism and pharmacokinetics" made a more in-depth study on the pharmacodynamics and drug metabolism of piperaquine in the human body, and found that piperaquine has 5 main metabolites after being absorbed and utilized by the human body, one of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K9/00A61P33/06
CPCY02A50/30
Inventor 宓穗卿刘昌辉陈沛泉黄小桃王宁生
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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