Application of ieodoglucomides B to prepare monoamine oxidase (MAO) inhibitor

A technology of monoamine oxidase and inhibitor, which is applied in the application field of preparing monoamine oxidase MAO inhibitor, and achieves the effect of strong inhibitory activity and outstanding substantive characteristics

Inactive Publication Date: 2016-02-03
ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But because "cheesereaction" causes hi...

Method used

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  • Application of ieodoglucomides B to prepare monoamine oxidase (MAO) inhibitor
  • Application of ieodoglucomides B to prepare monoamine oxidase (MAO) inhibitor
  • Application of ieodoglucomides B to prepare monoamine oxidase (MAO) inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1: Preparation of IeodoglucomidesB tablet of the compound involved in the present invention:

[0012] Take 5 grams of compound Ieodoglucomides B and add 195 grams of dextrin, mix well, and prepare 1000 tablets with a conventional tablet machine.

Embodiment 2

[0013] Example 2: Preparation of the compound IeodoglucomidesB capsule of the present invention:

[0014] Take 5 grams of compound Ieodoglucomides B and add 195 grams of starch, mix them, and encapsulate them to make 1000 tablets.

[0015] The following pharmacodynamic experiments will further illustrate its drug activity.

[0016] The compound IeodoglucomidesB is used to detect the inhibitory activity of MAO-A and MAO-B by fluorescent probe method,

[0017] The described method follows the following steps:

[0018] Dissolve the sample to be tested in DMSO to prepare a series of samples with a concentration gradient. Take 4ul of MAO (10mg / ml), boric acid buffer (PH=8.4), 50ulBSA (50mg / ml), add the sample solution to be tested, mix well, react in a water bath at 30~38℃ for 3h, then add probe 7- (3-Aminopropoxy) coumarin 2ul (50mmol / ml), the final concentration of inhibitor is 0~10-2mmol / l, and the mixture is reacted in a water bath at 30±5℃ for 12h, using a fully functional fluorescenc...

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Abstract

The invention provides application of ieodoglucomides B to prepare a monoamine oxidase (MAO) inhibitor, and compared with a known monoamine oxidase inhibitor, the monoamine oxidase (MAO) inhibitor is greatly improved in inhibition activity and selectivity on MAO-A and MAO-B. The related purpose of ieodoglucomides B to prepare the monoamine oxidase (MAO) inhibitor is disclosed for the first time. Because the l type belongs to a brand-new framework type and the inhibition activity of the inhibitor on monoamine oxidase (MAO) is unexpected, there is not the possibility that other compounds give any enlightenment, the technical scheme possesses prominent substantive features, and also treatment on monoamine oxidase (MAO) imbalance related diseases obviously possesses notable progress.

Description

Technical field [0001] The invention relates to a new application of the compound IeodoglucomidesB, and particularly relates to the application of IeodoglucomidesB in the preparation of monoamine oxidase MAO inhibitors. Background technique [0002] Since the discovery of the anti-tuberculosis drug Isoniazid as a potential MAO inhibitor, the research on MAO inhibitors has become a hot spot. Isonicotinic hydrazide became the first MAO inhibitor, because it was discovered that this type of MAO inhibitor containing a hydrazine structure can also inactivate P450s and cause liver toxicity; also studied non-hydrazine MAO inhibition represented by tranylcypromine Agents, this type can be called the second generation. But because "cheesereaction" triggers high blood pressure, its application is limited. Therefore, it is quite necessary and urgent to develop a newer and more efficient monoamine oxidase inhibitor. [0003] The compound IeodoglucomidesB involved in the present invention is...

Claims

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Application Information

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IPC IPC(8): A61K31/7028A61P43/00
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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