Application of 4-cinnamyl-3-hydroxyl pyrrolidone compound in preparation of medicine for treating diabetes mellitus

The technology of a diabetes drug and compound is applied in the application field of 4-cinnamyl-3-hydroxypyrrolidone compound, preparation and treatment of diabetes drug, can solve problems such as inability to completely cure, and achieves improvement of oral glucose tolerance and insulin sensitivity Effect

Pending Publication Date: 2022-03-01
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the anti-diabetic drugs being clinically used are mainly aimed at improving symptoms and cannot completely cure the disease

Method used

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  • Application of 4-cinnamyl-3-hydroxyl pyrrolidone compound in preparation of medicine for treating diabetes mellitus
  • Application of 4-cinnamyl-3-hydroxyl pyrrolidone compound in preparation of medicine for treating diabetes mellitus
  • Application of 4-cinnamyl-3-hydroxyl pyrrolidone compound in preparation of medicine for treating diabetes mellitus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1. Acquisition of compounds XJ0240-XJ0245

[0059] The compound can be purchased from Compound Handling B.V. (Trade name: Specs), whose company address is Bleiswijkseweg 55, 2712PB Zoetermeer, The Netherlands, online shopping address: https: / / www.specs.net / .

[0060]

[0061]

Embodiment 2

[0062] Example 2. The acquisition of compound XJ2046-XJ0273

[0063] Compounds are commercially available from ChemDiv Inc., 12760 High Bluff Drive, Suite 370 San Diego, CA 92130 USA. Online shopping address: https: / / www.chemdiv.com / .

[0064]

[0065]

[0066]

[0067]

[0068] 2. Evaluation of the biological activity of the compound

experiment example 1

[0069] Experimental example 1. Determination of HDAC3 / NCoR1 enzyme inhibitory activity

[0070] 1. Experimental method

[0071] Enzyme inhibitory activity was determined by Enzo's HDAC3 / NCoR1 Fluorometric Drug Discovery Kit. Reactions were performed in 96-well plates. Dilute the compound to 5×C with Assay Buffer II Final The sample buffer and the vehicle DMSO were added to Buffer II in the same volume as a negative control. Add 25 μL Assay Buffer II (blank control), or 10 μL negative control, or sample buffer (positive control TSA, or test compound) to each well; dilute the enzyme recombinant complex HDAC3 / NCoR1 to 3.3×C with Assay Buffer II Final Enzyme working solution, added to each well (15μL / well, except blank control); Dilute the substrate FLUOR DE with Assay Buffer -SIRT1 to 2×C Final Substrate working solution, and preheated to 37°C, add 25 μL of preheated substrate working solution to all wells, start the reaction after mixing well, incubate at 37°C for 15-20 mi...

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PUM

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Abstract

The invention belongs to the technical field of diabetes treatment medicines, and particularly relates to application of a 4-cinnamyl-3-hydroxyl pyrrolidone compound in preparation of a medicine for treating and / or preventing diabetes. The compound is shown as a formula (1), wherein R1 is selected from hydrogen, halogen, C1-8 alkoxy, hydroxyl and nitryl; r2 is selected from hydrogen, halogen, C1-8 alkyl, C1-8 alkoxy, halogenated C1-8 alkyl and carboxyl; the substitution positions of R1 and R2 are selected from monosubstitution at any position and polysubstitution of the same or different groups. The 4-cinnamyl-3-hydroxyl pyrrolidone compound disclosed by the invention has the effects of remarkably promoting pancreatic beta cells to secrete and synthesize insulin, and improving oral glucose tolerance and insulin sensitivity, and can be used for preparing novel medicines for treating and / or preventing diabetes mellitus.

Description

technical field [0001] The invention belongs to the technical field of drugs for treating diabetes, and in particular relates to the application of 4-cinnamyl-3-hydroxypyrrolone compounds in the preparation of drugs for treating diabetes. Background technique [0002] Diabetes is a major chronic non-communicable disease of human beings, which seriously threatens human health. Most of the antidiabetic drugs being clinically used mainly improve the symptoms, but cannot completely cure the disease. Therefore, there is an urgent need to develop anti-diabetic drugs with new mechanisms of action and new structural types. [0003] The latest research shows that selective inhibition of histone deacetylase subtype 3 (HDAC3) can protect islet β cells and promote insulin secretion, thereby effectively reducing blood sugar levels in diabetic rats without affecting the normal differentiation of human megakaryocytes , can reduce the risk of thrombocytopenia caused by non-selective inhib...

Claims

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Application Information

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IPC IPC(8): A61K31/402A61P3/10
CPCA61K31/402A61P3/10
Inventor 吴松申竹芳夏杰环奕雷蕾白国良
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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