Glycogen phosphorylase inhibitor and preparation method and application thereof

A phosphorylase inhibitor, glycogen phosphorylase technology, applied in the field of drug synthesis, can solve the problem of limited hypoglycemic effect

Inactive Publication Date: 2016-10-26
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the hypoglycemic eff

Method used

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  • Glycogen phosphorylase inhibitor and preparation method and application thereof
  • Glycogen phosphorylase inhibitor and preparation method and application thereof
  • Glycogen phosphorylase inhibitor and preparation method and application thereof

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Embodiment 1

[0038] The preparation of a kind of glycogen phosphorylase inhibitor in this embodiment, the specific preparation steps are as follows:

[0039] (1) Synthesis of (E)-3-{2-[(4-tert-butoxycarbonylphenyl)azido]phenyl}propionic acid:

[0040] (E)-3-(nitrophenyl)acrylic acid (10.0g, 52.0mmol) was dissolved in water (500mL), NaOH (4.1g, 39mmol) and 10%Pd / C (0.5g) were added, hydrogenated at room temperature and atmospheric pressure overnight. The reactant was filtered to remove Pd / C, and the solvent was evaporated under reduced pressure to obtain a white powdery solid crude product (7.5 g, 87%). This crude product was dissolved in a mixed solvent of water (200 mL) and dichloromethane (300 mL), and potassium hydrogen persulfate (Oxone, 55.3 g, 90.0 mmol) was added, and stirred at room temperature for 2 h. The organic phase of dichloromethane was collected by extraction, the aqueous phase was extracted with dichloromethane, the organic phases were combined, dried over anhydrous sodi...

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Abstract

The invention belongs to the technical field of drug synthesis and discloses a glycogen phosphorylase inhibitor and a preparation method and application thereof. The gGlycogen phosphorylase inhibitor has a structural general formula shown as a formula (1) or pharmaceutically-acceptable salt or ester, wherein each of X1, X2, X3 and X4 is a carbon atom connecting group, or one of X1, X2, X3 and X4 is a nitrogen atom connecting group while each of the others is a carbon atom connecting group; R is H, halogen, hydroxyl, cyan, alkyl of C1-6, alkoxy of C1-6, trifluromethyl, vinyl or acetylenyl. The glycogen phosphorylase inhibitor of a novel structure has inhibiting effect on glycogen phosphorylase, is equivalent to PSN-357 in glycogenolysis inhibiting effect on a cell level and can be used for preparing drugs for treating diabetes and complications thereof, hyperlipemia, hypertension and complications thereof, atherosis, obesity and metabolic syndrome.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to a glycogen phosphorylase inhibitor and its preparation method and application. Background technique [0002] Diabetes is the third chronic non-communicable disease that seriously threatens human health after tumors and cardiovascular diseases. At present, there are more than 92 million diabetic patients in my country, becoming the world's largest diabetic country, and about 97% of them belong to type 2 diabetes. For the treatment of type 2 diabetes, according to the different pharmacological mechanisms of drugs, it is divided into insulin and its similar drugs, insulin sensitizers, insulin secretagogues, and carbohydrate-reducing regulators. However, the hypoglycemic effect of these drugs is limited. With the deepening of people's understanding of the pathogenesis of diabetes, many new targets for the treatment of diabetes have been discovered, and new drugs ...

Claims

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Application Information

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IPC IPC(8): C07J43/00A61K31/58A61P3/10A61P3/06A61P9/12A61P9/10A61P3/04A61P3/00
CPCA61K31/58C07J43/00C07J43/003
Inventor 李晶张丽颖张雷
Owner SOUTH CHINA UNIV OF TECH
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