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Benzothiazole derivative, preparation method and application thereof

A technology of benzothiazole and derivatives is applied in the field of medical technology to achieve the effects of promoting yeast growth, enhancing metabolic growth and reducing fasting blood sugar

Active Publication Date: 2013-04-17
斯芬克司药物研发(天津)股份有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Through searching, it is found that whether benzothiazole derivatives can activate SIRT1 through yeast Sir2 gene screening and mouse in vivo testing to prevent diabetes and its complications has not been reported in the literature so far.

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

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Embodiment Construction

[0042] 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.

[0043] 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.

[0044] The principle of the present invention is based on the high homology between yeast Sir2 and mammalian SIRT1, and proves that the benzothiazole derivative JHJ2 can promote the growth of yeast, enhance its metabolic activity, and can significantly reduce the C57 BL / 6J fed with high-fat feed for a long time. Plasma triglycerides, total cholesterol and high-density lipoprotein in mice can reduce systolic and diastolic blood pressure of model mice, reduce fasting blood glucose o...

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Abstract

The invention relates to a benzothiazole derivative, a preparation method and an application thereof, wherein the benzothiazole derivative is 2-m-aniline benzothiazole-1H-pyrazole-3-formamide, and the structural formula of the benzothiazole derivative is shown in the description. The benzothiazole derivative disclosed by the invention can accelerate the growth of saccharomycetes, strengthen the metabolic activity of the saccharomycetes, obviously reduce the plasma triglyceride, the total cholesterol and the high-density lipoprotein of C57 BL / 6J mice fed with high-fat feedstuff, reduce the systolic pressure and the diastolic pressure of model mice, reduce the fasting blood glucose of the model mice, improve the sugar tolerance of the mice, affect the expression of SIRT1 and relevant genes (FOXO1, P53, PPAB gamma and PGC-1 alpha), and obviously improve the sugar and fat metabolism of diabetic model mice. Therefore, the benzothiazole derivative can be applied to preparing medicines for preventing and treating diabetes mellitus and complications of the diabetes mellitus.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to thiazole derivatives, especially the compound 2-m-anilinobenzothiazole-1H-pyrazole-3-carboxamide and its preparation method and its use as a sirtuin agonist Application, 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 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 com...

Claims

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Application Information

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IPC IPC(8): C07D417/12A61P3/10A61P3/06
Inventor 花尔并贾绍龙王莹莹
Owner 斯芬克司药物研发(天津)股份有限公司
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