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Dastorin primary alkylate derivative and its pharmaceutical composition, its preparation method and application

A technology of diastrin and alkyd ester, which is applied in the field of diasterin primary alkylate derivatives as a class of potent pancreatic lipase inhibitors, and can solve the problem of unseen diasterin primary alcohol Reports on the activity of ester derivatives and other issues

Inactive Publication Date: 2017-06-20
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] So far, there is no report on the first grade alkylate derivatives of stasis and its activity in the prior art

Method used

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  • Dastorin primary alkylate derivative and its pharmaceutical composition, its preparation method and application
  • Dastorin primary alkylate derivative and its pharmaceutical composition, its preparation method and application
  • Dastorin primary alkylate derivative and its pharmaceutical composition, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] 1 H-and 13 C-NMR is measured by Bruker AVANCE III-600, DRX-500 or AM-400, internal standard is TMS, wherein 1 H NMR measured at 400MHz, 500MHz and 600MHz, 13 C NMR was measured at 100MHz, 125MHz and 150MHz; mass spectrometry HREI-MS and EI-MS were determined by Finnigan-MAT90 mass spectrometer; HRESI-MS and ESI-MS were determined by API QSTAR Pulsari mass spectrometer; rotary evaporator: Buchi R-200 , R-201; DLSB5110 type low temperature reaction coolant circulation pump, IKARCT basic (safety control type) heating magnetic stirrer.

[0038] Column chromatography material: silica gel (80-100 mesh and 200-300 mesh) and prefabricated GF for column chromatography 254All TLC plates were produced by Qingdao Ocean Chemical Factory; Sephadex LH-20 was produced by Amersham Biosciences, Sweden; Chromatorex C-18 (40-75 μm) was produced by Fuji Silysia Chemicals, Japan. HPLC: Agilent1100, Zorbax SB-C18column, 5μm, 4.6mm×150mm; Prep-HPLC: Agilent1200, Zorbox SB-C18column, 5μm, 9...

Embodiment 2

[0098] In vitro experiments on the inhibition of pancreatic lipase by the compounds of the present invention:

[0099] 1. Determination of Drugs and Compounds

[0100] Determination compound is the first grade alkylate derivative of vibralactone gained in Example 1, totally 43 compounds; Positive drug is Orlistat (Orlistat, N-Formyl-L-leucine (1S)-1- [[(2S,3S)-3-hexyl-4oxo-2-oxetanyl]methyl]dodecyl ester) was purchased from Sigma; the compound and Orlistat were dissolved in dimethylsulfoxide (DMSO) and stored at 4°C.

[0101] 2. Reagents and solutions

[0102] (1) Reagents

[0103] Porcine pancreatic lipase (PPL) was purchased from Aladdin Reagent Company; p-nitrophenyl butyrate (p-NPB) and Tris were purchased from Sigma Company; D-PBS was purchased from Hyclone Company; anhydrous calcium chloride was purchased from Chengdu Kelong Chemical Reagent factory products.

[0104] (2) Solution

[0105] Tris buffer containing 100mM Tris, 5mM CaCl 2 , pH value is 7.0, and stored ...

Embodiment 3

[0122] The compound was prepared according to Example 1, and excipients were added according to the weight ratio of compound crystals and excipients at a ratio of 1:1, and then granulated and compressed into tablets.

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to a first-grade alcohol acid ester derivative (represented by a formula I as shown in the specification) of vibralactone, a pharmaceutical composition taking the first-grade alcohol acid ester derivative of the formula I or pharmaceutically acceptable salt of the first-grade alcohol acid ester derivative as active components, preparation methods of the first-grade alcohol acid ester derivative and the pharmaceutical composition and application of the first-grade alcohol acid ester derivative and the pharmaceutical composition in preparation of medicines for preventing and treating obesity and other metabolic diseases, such as diabetes.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a class of strong pancrelipase inhibitors, which can inhibit the activity of enzymes by combining with pancrelipase, and prevent the hydrolysis of triglycerides Absorbed free fatty acids and monoacylglycerols prevent them from being absorbed, thereby reducing calorie intake and controlling body weight. Background technique [0002] Obesity is a disease caused by disorders of appetite, energy intake, and metabolic regulation. It has obvious correlations with diabetes, cardiovascular disease, fatty liver, and certain tumors. It has become a major killer of human health. Therefore, how to effectively reduce obesity has become an important research topic facing many countries. Dietary fat intake is one of the main causes of obesity. The main lipid component in food is triglycerides, which are hydrolyzed into corresponding monoglycerides and fatty acids before being absorbed. In...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D305/14C07D409/12C07D407/12C07D405/12A61K31/365A61K31/443A61K31/381A61K31/4025A61P3/04A61P3/10
CPCC07D305/14C07D405/12C07D407/12C07D409/12
Inventor 刘吉开韦堃汪钢强白雪李正辉董泽军汪秋安陈贺平冯涛文春南
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI