Thiophene derivatives and their preparation and application in the preparation of medicines

A derivative and thiophene technology, applied to thiophene derivatives and their preparation and application in the preparation of medicines, can solve the problem of no literature report on the hypoglycemic effect, and achieve rich traditional Chinese medicine raw materials, reduce side effects, and large clinical applications. effect of value

Inactive Publication Date: 2016-07-06
SHANGHAI CHANGZHENG HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Modern pharmacological studies have shown that Eclipta and its extracts have various pharmacological activities such as hemostasis, liver protection, immune regulation, anti-inflammation, anti-tumor, anti-oxidation, anti-aging, and anti-hypoxia [Journal of Traditional Chinese Medicine, 1997, 6: 28-29; Journal of Guangxi University of Traditional Chinese Medicine, 2008, 11(1): 76-78], but the hypoglycemic effect has not been reported in the literature

Method used

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  • Thiophene derivatives and their preparation and application in the preparation of medicines
  • Thiophene derivatives and their preparation and application in the preparation of medicines
  • Thiophene derivatives and their preparation and application in the preparation of medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1 prepares thiophene derivatives

[0033] 15Kg of dried whole Eclipta chinensis, crushed, heated and refluxed with 150L of 80% ethanol for 3 times, 1 hour each time, combined the 3 extracts, and filtered to obtain the total filtrate. Take 200ml of the filtrate and concentrate under reduced pressure at 60°C to evaporate the solvent to obtain the total ethanol extract of Eclipta chinensis. The rest of the filtrate was concentrated under reduced pressure at 60°C until there was no alcohol smell, and suspended in 20L of water. Extract with petroleum ether (15L×3), ethyl acetate (15L×3), and n-butanol (15L×3) in sequence. Petroleum ether, ethyl acetate, and n-butanol layers were respectively concentrated under reduced pressure at 60°C to obtain 240 g of petroleum ether extract, 320 g of ethyl acetate extract, and 550 g of n-butanol extract.

[0034] Take 235g of petroleum ether extract, use normal phase silica gel (100-200 mesh) column chromatography, and use petr...

Embodiment 2

[0054] Example 2 In vitro hypoglycemic activity experiment

[0055] 1. Experimental drugs:

[0056] The total ethanol extract, petroleum ether fraction, ethyl acetate fraction, n-butanol fraction, and compounds 1-9 of Eclipta chinensis prepared in Example 1.

[0057] 2. Reagents and materials:

[0058] DPP-IV (dipeptidyl peptidase) was derived from the plasma of healthy volunteers; MouseTNF-α Elisa kit (BioLegend, SanDiego, USA, commercially available); DiprotinA (dipeptidin) (EnzoLifeSciences, Inc., USA, commercially available) ); other reagents (analytical grade, Sinopharm Chemical Reagent Co., Ltd., commercially available).

[0059] 3. Experimental equipment:

[0060] Automatic microplate reader (Elx800, Biotek); 96-well cell culture plate (Costar).

[0061] 4. Experimental method:

[0062] The sample to be tested was dissolved in DMSO (dimethyl sulfoxide) to obtain a stock solution of 10 mg / mL, and then tested with a concentration of 6 μg / mL. DiprotinA (distatin A) w...

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Abstract

The invention provides a thiophene derivative, which includes a compound 1, a compound 2, a compound 3, a compound 4, a compound 5, a compound 6, a compound 7, a compound 8, and a compound 9. The structural formulas are shown as the specification. The compounds are prepared by extraction from Yerbadetajo Herb. The result of in vitro hypoglycemic activity experiment shows that the thiophene compounds 1-9 have significant inhibitory activity on DPP-IV, thus being applicable to preparation of drugs for prevention / treatment of diabetes. The invention provides new drugs for prevention / treatment of diabetes in clinical practice. Due to rich Chinese medicinal raw materials, the new drugs can reduce the side effects of chemical drugs, and have great clinical application value.

Description

technical field [0001] The invention relates to medicinal chemistry, specifically the preparation and application of designed drugs, in particular to thiophene derivatives and their preparation and application in the preparation of drugs. Background technique [0002] According to the data provided by the International Diabetes Federation (IDF), there were about 366 million diabetic patients in the world in 2011, and it is estimated that by 2030, the number of diabetic patients will exceed 552 million (Diabetes Research and Clinical Practice, 2011, 94: 311-321). Diabetes has become a major public health problem worldwide. Studies have found that glucagon-like peptide-1 (GLP-1) and glucose insulinotropic polypeptide (GIP) can treat type II diabetes. Dipeptidyl peptidase (DPP-IV) is a serine protease, which is a key enzyme in the body that mainly promotes the degradation and inactivation of GLP-1 and intestinal inhibitory peptide, while GLP-1 and GIP can promote the secretion...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D333/16C07D333/22A61K31/381A61P3/10
CPCC07D333/16C07D333/22
Inventor 陈万生习峰敏吴志军黎春彤韩军梁凤英
Owner SHANGHAI CHANGZHENG HOSPITAL
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