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Geniposide derivative with xanthine oxidase inhibitory activity as well as preparation method and application of geniposide derivative

A technology of xanthine oxidase and geniposide, which is applied in the field of geniposide derivatives and preparation, can solve problems such as non-use, achieve the effect of improving biological activity, low raw material price, and inhibiting xanthine oxidase activity

Active Publication Date: 2022-04-12
VEGETABLE RES INST OF SHANDONG ACADEMY OF AGRI SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, acute liver damage caused by allopurinol has also been reported clinically, so allopurinol is generally not used in patients with hyperuricemia who also suffer from liver disease

Method used

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  • Geniposide derivative with xanthine oxidase inhibitory activity as well as preparation method and application of geniposide derivative
  • Geniposide derivative with xanthine oxidase inhibitory activity as well as preparation method and application of geniposide derivative
  • Geniposide derivative with xanthine oxidase inhibitory activity as well as preparation method and application of geniposide derivative

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Experimental program
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Embodiment 1

[0035] The preparation method of geniposide derivatives with xanthine oxidase inhibitory activity: First, 200 mg of geniposide (about 0.51 mmol) was dissolved in 3 mL of dichloromethane, placed in a two-necked flask, and added to the flask 10ml 4% NaOH solution, temperature controlled to 65°C. After reacting for 3 h, distill under reduced pressure and spin dry the water. Add 5ml of acetic anhydride and 1ml of triethylamine, and stir overnight at room temperature. After the reaction, distill under reduced pressure, spin the solution to dryness, add 0.12 mml oxalyl chloride, and react at room temperature for 3 h. After the reaction, distill under reduced pressure, spin the solution to dryness, add 50.7 mg (about 0.37 mmol) of 4-mercaptopyridine under ice bath, react at room temperature, and track the reaction by TLC. After the reaction, the reaction solution was concentrated and purified through a neutral alumina column. The eluent was petroleum ether: ethyl acetate (8:1, 5:1,...

Embodiment 2

[0041]The preparation method of geniposide derivatives with xanthine oxidase inhibitory activity, first dissolve 200 mg geniposide (about 0.51 mmol) in 3 mL methylene chloride, place in a two-necked flask, add 10ml 4% NaOH solution, temperature controlled to 65°C. After reacting for 3 h, distill under reduced pressure and spin dry the water. Add 5ml of acetic anhydride and 1ml of triethylamine, and stir overnight at room temperature. After the reaction, distill under reduced pressure, spin the solution to dryness, add 0.12 mmol oxalyl chloride, and react at room temperature for 3 h. After the reaction, distill under reduced pressure, spin the solution to dryness, add 41.5 mg (about 0.37 mmol) of 2-mercaptothiazoline under ice bath, react at room temperature, and track the reaction by TLC. After the reaction, the reaction solution was concentrated and purified through a neutral alumina column. The eluent was petroleum ether: ethyl acetate (8:1, 5:1, 3:1, 2:1, 1:1), and separa...

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Abstract

The invention belongs to the field of compound synthesis, and particularly relates to a geniposide derivative with xanthine oxidase inhibitory activity as well as a preparation method and application of the geniposide derivative. The geniposide derivative has a molecular structure shown in the specification. According to the invention, a novel geniposide derivative is synthesized, and the geniposide derivative has an obvious effect of inhibiting the activity of xanthine oxidase; the geniposide is subjected to structural modification, so that the biological activity of the geniposide can be greatly improved, and the geniposide has important practical significance on research and development of novel uric acid reducing drugs; according to the geniposide derivative with the xanthine oxidase inhibitory activity, related structural modification is carried out by taking geniposide as a raw material, the synthesis method is simple, the raw material price is low, and the structure is novel.

Description

technical field [0001] The invention belongs to the field of compound synthesis, and specifically relates to a geniposide derivative with xanthine oxidase inhibitory activity, a preparation method and an application thereof. Background technique [0002] Hyperuricemia is a disease that seriously endangers human health. From a clinical point of view, patients with hyperuricemia can be diagnosed when the serum uric acid concentration in men exceeds 420 μM and in women exceeds 360 μM. Due to the excessive intake of high-purine foods, the incidence of hyperuricemia in my country is increasing year by year, and the age of onset is significantly younger. As of 2019, the number of patients with hyperuricemia in my country has reached 200 million, making it the second largest metabolic disease after diabetes. Up to now, there have been no new urate-lowering drugs available for nearly ten years. Therefore, there is an urgent need to find novel, safe and effective uric acid-lowering...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/04C07H1/00A61P19/06
Inventor 刘超陈家树孙金月王目旋郭溆王青
Owner VEGETABLE RES INST OF SHANDONG ACADEMY OF AGRI SCI
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