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Benzoxazole derivative as well as preparation method and application thereof

A technology of benzoxazole and methyl benzoxazole is applied in the field of medicine to achieve the effects of preventing and treating hyperglycemia, promoting growth activity and enhancing metabolic growth

Inactive Publication Date: 2014-09-03
TIANJIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Through searching, it is found that whether benzoxazole derivatives can overactivate SIRT1 through yeast Sir2 gene screening and fruit fly testing can play a role in preventing and treating diabetes and its complications, so far there has been no literature report

Method used

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  • Benzoxazole derivative as well as preparation method and application thereof
  • Benzoxazole derivative as well as preparation method and application thereof
  • Benzoxazole derivative as well as preparation method and application thereof

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Embodiment Construction

[0045] 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.

[0046] 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.

[0047] The principle of the present invention is based on the high homology between yeast SIR2 and mammalian SIRT1, and proves that benzoxazole derivatives can promote the growth of yeast, and can significantly improve the activities of SOD, Cu-ZnSOD and CAT in Drosophila, and reduce MDA The content of SIRT1 may activate SIRT1 and affect the expression of SIRT1 and related genes.

[0048] One, a kind of benzoxazole derivative and preparation method thereof, the steps are as follo...

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Abstract

The invention relates to a benzoxazole derivative. The benzoxazole derivative is (5-methylbenzoxazole-2-phenyl)-3'-methoxybenzamide, can be applied to silent information regulator agonist SIRT1 and preparation of medicaments for reducing, improving, preventing and treating II-type diabetes mellitus or hyperglycemia, abnormal glucose tolerance, dyslipidemia and complications caused by those diseases due to the II-type diabetes mellitus. In-vitro saccharomycete experiments prove that the SIRT1 agonist, such as benzoxazole derivative (5-methylbenzoxazole-2-phenyl)-3'-methoxybenzamide can be used for promoting the growing activity of saccharomycetes, reinforcing metabolic growth, improving the activity of SOD (superoxide dismutase), Cu-Zn SOD and CAT (chloramphenicol acetyl transferase) in the body of drosophila melanogaster, reducing the content of MDA (methylene dioxyamphetamine), and increasing the expression quantity of anti-oxidation gene CAT mRNA (messenger ribonucleic acid).

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a benzoxazole derivative and its preparation method and application. 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 triglyceride or hypercholesterolemia. Hyperlipidemia is one of the main reasons for insulin resistance and islet β cell dysfunction. Commonly used hypoglycemic drugs include: insulin, sulfonylurea drugs, non-sulfonylurea insulin secretagogues, biguanide hypoglycemic drugs, insulin sensitizers, etc. Strong, damage to liver, kidney and other organs, some diabetics show obvious resistance to insulin. Therefore, finding new safe and effective anti-diabetic drugs by synthesizing new compounds and discovering new protein targets is an effect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D263/57A61P3/10A61P3/06A61P35/00
CPCC07D263/57
Inventor 花尔并王轶菲黄杰王浩敖军礼俞悦
Owner TIANJIN UNIV OF SCI & TECH
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