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2-undecyl-3-methyl-hydroxyl-quinoline compound as well as preparation method, pharmaceutical composition and use thereof

The technology of a compound, merolinol, which is applied in the field of medicine, can solve the problems of not having the effect of inhibiting tumor angiogenesis and poor resistance to Helicobacter pylori, and achieve the goal of easy industrialization and application, overcoming technical defects, and strong anti-Helicobacter pylori effect Effect

Inactive Publication Date: 2014-03-26
CHONGQING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The 1-position N of the quinolinone structure described in CN1255853 is hydroxylated, the 2-position is substituted by 2-trans-nonenyl, and the 4-position is a ketone group. It is prepared by a fermentation method. The invention inhibits tumor angiogenesis

Method used

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  • 2-undecyl-3-methyl-hydroxyl-quinoline compound as well as preparation method, pharmaceutical composition and use thereof
  • 2-undecyl-3-methyl-hydroxyl-quinoline compound as well as preparation method, pharmaceutical composition and use thereof
  • 2-undecyl-3-methyl-hydroxyl-quinoline compound as well as preparation method, pharmaceutical composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1, preparation and synthesis of merolinol compound:

[0054] The preparation of 2-undecyl-3-methyl-4(1H)-merolinol compound specifically comprises the following steps:

[0055] 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 triethylamine, 60-80ml of dichloromethane, stir and react at 10-30°C for 4-20 hours, add Take 60-100ml of saturated ammonium chloride solution, take the organic phase, concentrate under reduced pressure, and conduct silica gel column chromatography on the residue to collect the target object, concentrate under reduced pressure, and dry to obtain lauroamidopropiophenone;

[0056] Step 2: Put 11mmol of laurylaminopropiophenone in step 1 into a 250ml double-necked round bottom flask, add 30-40mmol of sodium ethylate, 180-240ml of absolute ethanol, reflux for 12-36 hours, concentrate under reduced pressure to recover ethanol, add water 100-200ml...

Embodiment 2

[0060] Embodiment 2, the method for preparing merolinol tablet preparation:

[0061] With the merolinol prepared in Example 1 as raw material, prepare merolinol tablet, the formula of 1000 tablets is as follows:

[0062] Merlinol (as C 21 h 31 NO meter) Starch and other accessories 100 150

[0063]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

[0064] Embodiment 3, the method for preparing merolinol capsules:

[0065] Taking the merolinol compound prepared by Preparation Example 1 as raw material, prepare merolinol capsules, the formula of 1000 capsules is as follows:

[0066] Merlinol (as C 21 h 31 NO meter) Starch and other accessories 100 150

[0067] 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.

[0068] Biological test 1: antibacterial effect of merolinol:

[0069] 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.) The anti-clinical isolates of Helicobacter pylori SW-2 and standard strains were tested (Table 1), and the test results indicated that the inhibitory effect of merolinol on clinic...

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Abstract

The invention provides a 2-undecyl-3-methyl-hydroxyl-quinoline compound, a preparation method of the 2-undecyl-3-methyl-hydroxyl-quinoline compound, a pharmaceutical composition containing the 2-undecyl-3-methyl-hydroxyl-quinoline compound and use of the 2-undecyl-3-methyl-hydroxyl-quinoline compound and belongs to the technical field of medicine. Particularly, the invention provides a compound shown in a formula I and a use of the pharmaceutical composition of the compound in the preparation of medicine for preventing and / or treating gastritis and tumor caused by Helicobacter Pylori. The I compound provided by the invention not only has relatively high selective inhibition effect on the Helicobacter Pylori, but also has obvious inhibition effect on tumor angiogenesis, so that a possibility is provided for developing new anti-tumor medicine and medicine for treating the gastritis caused by the Helicobacter Pylori.

Description

technical field [0001] The invention provides a merolinol compound, a preparation method thereof, a pharmaceutical composition containing them and applications, belonging 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 for tumors such as gastric 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 population 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 a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/233A61K31/47A61P1/04A61P31/04A61P35/00
CPCC07D215/233
Inventor 郑一敏胥秀英王锐李敖刘红张心蕊陈海芹张云玲
Owner CHONGQING UNIV OF TECH
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