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Benzimidazole derivative, and preparation method and application thereof

A technology of benzimidazole and derivatives is applied in the fields of benzimidazole derivatives and their preparation and application, and achieves the effects of improving glucose tolerance, reducing fasting blood sugar, and promoting yeast growth

Active Publication Date: 2013-02-27
斯芬克司药物研发(天津)股份有限公司
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0005] Screening self-developed benzimidazole derivatives to activate SIRT1 through yeast Sir2 gene and mouse in vivo tests, so as to find high-efficiency and low-toxic drug candidates for preventing and treating diabetes and its complications, which has not been reported in the literature so far

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  • Benzimidazole derivative, and preparation method and application thereof
  • Benzimidazole derivative, and preparation method and application thereof
  • Benzimidazole derivative, and preparation method and application thereof

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Embodiment Construction

[0041] The present invention will be further described in detail below through the specific examples, the following examples are only descriptive, not restrictive, and cannot limit the protection scope of the present invention with this.

[0042] The reagents used in this example are all commercially available products unless otherwise specified; the methods used are all conventional methods unless otherwise specified; the instruments used are all conventional instruments unless otherwise specified.

[0043] The principle of the present invention is based on the high homology between yeast Sir2 and mammalian SIRT1, and proves that benzimidazole derivatives, that is, compound 2-m-anilinobenzimidazole-1H-pyrazole-3-carboxamide (JHJ3 for short) can promote The yeast grows, enhances its metabolic activity, and can significantly reduce the plasma triglyceride, total cholesterol and high-density lipoprotein of C57 BL / 6J mice fed with high-fat diet for a long time, and reduce the systol...

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Abstract

The invention relates to a benzimidazole derivative 2-m-phenylaminobenzimidazolyl-1H-pyrazolyl-3-formamide of which the structural formula is disclosed in the specification. The benzimidazole derivative can promote growth of microzyme, enhance the metabolic activity of the microzyme, obviously lower the plasma triglyceride, total cholesterol and high density lipoprotein of a C57 BL / 6J mouse which is fed by high-fat feed for a long time, lower the contractive pressure and diastolic pressure of the model mouse, lower the fasting blood-glucose of the model mouse, improve the sugar tolerance of the mouse, influence the expression of SIRT1 and related genes (FOXO1, P53, PPARgamma and PGC-1alpha), and obviously improve the metabolism of glucose and fat; and therefore, the benzimidazole derivative can be used for preparing medicines for preventing and treating diabetes and complications thereof.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to imidazole derivatives, especially the compound 2-m-anilinobenzimidazole-1H-pyrazole-3-carboxamide and its application as a sirtuin agonist. Application in the preparation of drugs for alleviating, improving, preventing and treating type II diabetes or complications caused by diabetes, including hyperglycemia, abnormal glucose tolerance, abnormal lipid metabolism and the complications caused by the above-mentioned diseases. Background technique [0002] Type II diabetes accounts for 90% of total diabetes, and its main pathogenesis is insulin resistance, pancreatic β-cell failure and insulin secretion disorder. Patients with type II diabetes are often accompanied by obesity, high blood pressure, high triglycerides or hypercholesterolemia. Hyperlipidemia is one of the main causes of insulin resistance and pancreatic β-cell dysfunction. Currently commonly used hypoglyce...

Claims

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Application Information

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IPC IPC(8): C07D403/12A61K31/4184A61P3/10A61P3/00
Inventor 花尔并贾绍龙王秋月
Owner 斯芬克司药物研发(天津)股份有限公司
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