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Quinolinone compound, preparation method and pharmaceutical composition of quinolinone compound and application of pharmaceutical composition

A compound, quinolinone technology, applied in the field of medicine, achieves strong anti-Helicobacter pylori effect and overcomes technical defects

Inactive Publication Date: 2013-05-15
CHONGQING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it cannot be used to solve the problem of treating digestive system diseases caused by Helicobacter pylori

Method used

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  • Quinolinone compound, preparation method and pharmaceutical composition of quinolinone compound and application of pharmaceutical composition
  • Quinolinone compound, preparation method and pharmaceutical composition of quinolinone compound and application of pharmaceutical composition
  • Quinolinone compound, preparation method and pharmaceutical composition of quinolinone compound and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1, preparation and synthesis of merlinone compound:

[0044] The preparation of 2-undecyl-3-methyl-4(1H)-quinolinone compound specifically comprises the following steps:

[0045] Step 1: Take 13mmol of o-aminopropiophenone and 20mmol of lauroyl chloride, put them in a 250ml double-necked round bottom flask, add 18mmol of pyridine, 60-80ml of dichloromethane, stir and react at 10-30°C for 4-20 hours, add saturated chlorine Ammonium chloride solution 60-100ml, take the organic phase, concentrate under reduced pressure, conduct silica gel column chromatography on the residue, collect the target object, concentrate under reduced pressure, and dry to obtain lauroamidopropiophenone;

[0046] Step 2: Put 11 mmol of laurylaminopropiophenone in step 1 into a 250 ml double-neck round bottom flask, add 30-40 mmol of sodium tert-butyl alkoxide, 180-240 ml of absolute ethanol, reflux for 12-36 hours, concentrate and recover under reduced pressure Ethanol, add 100-200ml ...

Embodiment 2

[0050] Embodiment 2, the method for preparing merlinone tablet preparation:

[0051] The merolinone prepared in Example 1 is used as raw material to prepare merolinone tablets, and the formula of 1000 tablets is as follows:

[0052] Merlinone (as C 21 h 31 NO meter)

[0053] Mix the raw materials and auxiliary materials, grind them into fine powder, pass through a 100-mesh sieve, take the amount according to the formula, press into tablets, and pack.

Embodiment 3

[0054] Embodiment 3, the method for preparing merlinone capsule:

[0055] Taking the merolinone compound prepared by Preparation Example 1 as raw material, prepare merolinone capsules, the formula of 1000 capsules is as follows:

[0056] Merlinone (as C 21 h 31 NO meter)

Starch and other accessories

100

150

[0057] Mix the raw materials and auxiliary materials, grind them into fine powder, pass through a 100-mesh sieve, take the amount according to the formula, granulate and pack.

[0058] Biological test 1: antibacterial effect of merlinone:

[0059] According to the literature (Ibrahim M, Khan AA, Tiwari SK, et a1. Antimierobia activity of Sapindus mukorossi and Rheum emodi extracts against H. priori: in vitro and in vivo studies. World J Gastroenterol, 2006.14: 7136-7142.) method The effect of merlinone against clinically isolated Helicobacter pylori SW-2 and standard strains was tested (Table 1). Linmycin.

[0060] Table 1 MIC of...

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Abstract

The invention provides a novel quinolinone compound called after morpholine ketone of which the chemical structure is shown in formula I, the name is 2-undecyl-3-methyl-4(1H)-quinolinone and the chemical formula is C21H31NO. The invention also provides an application of a pharmaceutical composition of the compound in preparation of a medicament for preventing and / or treating a gastritis disease caused by helicobacter pylori. The N at a first site of the quinolinone is not hydroxylated, and the N at a second site of the quinolinone is substituted by undecyl. The quinolinone is completely synthesized. The compound I has a highly-selective inhibiting effect on the helicobacter pylori and can also be used as an efficient proton pump inhibitor, so that the probability of developing a new medicament for treating the gastritis disease caused by the helicobacter pylori is provided.

Description

technical field [0001] The invention provides a quinolinone compound, a preparation method thereof, a pharmaceutical composition containing them and an application, which belong to the technical field of medicine. Background technique [0002] Helicobacter pylori (Helicobacter pylori) is a Gram-negative Helicobacter that colonizes the gastric mucosa. It is an important pathogenic factor that causes chronic gastritis and peptic ulcer. Class I carcinogen in mucosa-associated lymphoid tissue lymphoma and gastric adenocarcinoma. The chronic infection rate of H. pylori in the population of the world is as high as more than 50%, and the rate of infected people in developing countries even reaches 70-90%. The 2001-2004 epidemiological survey of the Digestive Disease Branch of the Chinese Medical Association showed that the infection rate of Helicobacter pylori in my country was 40%-90%, with an average of 59%; the infection rate of children was 25%-59%, with an average of 40%, and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/233A61K31/47A61P1/04A61P31/04
Inventor 郑一敏王锐胥秀英张云玲陈海芹
Owner CHONGQING UNIV OF TECH
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