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Bisindolyl maleimide derivative and preparation method and application thereof

A compound and alkyl technology, applied in the field of bisindolemaleimide derivatives and their preparation and application, can solve the problems of uncertain curative effect, large toxic and side effects, etc.

Active Publication Date: 2016-11-23
OCEAN UNIV OF CHINA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although some progress has been made in the research of anti-DKD drugs, the existing clinical treatments such as controlling blood pressure, blood sugar, blood lipids and anti-inflammation can only delay the progress of DKD to renal failure, but cannot reverse or prevent the progression of the disease At the same time, it also faces problems such as uncertain curative effect and high toxicity and side effects (Curr Diabetes Rev 2005; 1:281-286), so it is urgent to develop new anti-DKD drugs that are safe and efficient for new targets

Method used

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  • Bisindolyl maleimide derivative and preparation method and application thereof
  • Bisindolyl maleimide derivative and preparation method and application thereof
  • Bisindolyl maleimide derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0195] [Example 1] Preparation of Compounds 1-196

[0196] Preparation of Compound 1

[0197] i) Preparation of 1-ethyl-3-indoleacetic acid (1a)

[0198] Under argon protection, add 4g sodium hydride (60% mass fraction, dispersed in paraffin) and 80mL tetrahydrofuran to a 250mL three-necked flask, stir and suspend at 0°C, add 30mL tetrahydrofuran-dissolved indole-3-acetic acid (3.5g, 20mmol), stirred for half an hour, added dropwise 30mL tetrahydrofuran dissolved iodoethane (5mL, 60mmol), slowly raised to room temperature, reacted overnight, lowered to 0°C, added dropwise 10 drops of methanol, and then added an appropriate amount of water to obtain Bright yellow solution, extracted with ethyl acetate, added concentrated hydrochloric acid to the aqueous layer and extracted again, combined the organic layers, and washed with anhydrous Na 2 SO 4 After drying and evaporating to dryness in vacuo, 3.87 g of product (1a) was obtained with a yield of 95.4% after silica gel column c...

Embodiment 2

[0840] [Example 2] activity test

[0841] 1. α-glucosidase inhibitory activity test

[0842] (1) Test method

[0843] Using p-nitrophenyl-α-D-glucopyranoside (PNPG) as substrate, the α-glucosidase inhibitory activity of some compounds was tested. PNPG is an analogue of maltose, which can generate yellow p-nitrophenol after the action of α-glucosidase, which can be directly used for detection by spectrophotometer. Specifically: firstly, the sample was dissolved in PBS sodium phosphate buffer solution (pH6.8) to make 5 concentrations; then 10 μL of sample solution, 20 μL of PBS solution, and 20 μL of 2.5 mM glucose were added to each well of a 96-well plate. Glycoside solution (dissolved in phosphate buffered saline solution), incubate in a 37°C incubator for 5 minutes. Dilute α-glucosidase to 0.2 U / mL with 0.01M PBS solution, add 10 μL from each well to the above test solution, incubate in a 37°C incubator for 15 minutes, and measure the concentration of α-glucosidase at 405...

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PUM

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Abstract

The invention provides a bisindolyl maleimide derivative and a preparation method and application thereof. The bisindolyl maleimide derivative has an excellent alpha-glucosidase inhibition effect and can be used for preventing and treating diabetes.

Description

Technical field: [0001] The present invention relates to a bisindole maleimide derivative and its preparation method and use. Background technique: [0002] With the changes in people's living habits and dietary structure, the incidence of diabetes is increasing year by year. According to the data released by WHO in 2011, about 4.6 million people die of diabetes-related diseases in the world every year, and the medical expenses for diabetes are as high as 465 billion US dollars. At present, there are nearly 100 million diabetics and about 340 million people with abnormal glucose metabolism in China. Diabetes has become the third leading killer after cancer and cardiovascular disease. [0003] Diabetes is divided into: type 1 diabetes (insulin-dependent diabetes) and type 2 diabetes (non-insulin-dependent diabetes), and more than 90% of patients belong to type 2 diabetes. Patients with type 2 diabetes do not need insulin therapy, and can regulate blood sugar with diet, and...

Claims

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Application Information

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IPC IPC(8): C07D403/14C07D401/14C07D487/14C07D498/22C07H15/26A61K31/404A61K31/7056A61K31/4178A61K31/5377A61K31/4439A61K31/407A61K31/496A61K31/454A61K31/5395A61P3/10A61P13/12
CPCC07D401/14C07D403/14C07D487/14C07H15/26C07H9/06A61P3/10A61P13/12
Inventor 朱伟明马红光王立平徐志红张亚鹏王乂刘培培郝杰杰
Owner OCEAN UNIV OF CHINA
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