Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of chukrasone A in the preparation of monoamine oxidase inhibitor drugs

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

Inactive Publication Date: 2016-04-27
重庆西南制药二厂有限责任公司
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because "cheesereaction" causes high blood pressure, its application is limited

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of chukrasone A in the preparation of monoamine oxidase inhibitor drugs
  • Application of chukrasone A in the preparation of monoamine oxidase inhibitor drugs
  • Application of chukrasone A in the preparation of monoamine oxidase inhibitor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Embodiment 1: the preparation of the compound ChukrasoneA tablet involved in the present invention:

[0013] Take 20 grams of compound Chukrasone A, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tablet press machine.

Embodiment 2

[0014] Embodiment 2: the preparation of the compound ChukrasoneA capsule involved in the present invention:

[0015] Get 20 grams of compound Chukrasone A, add conventional auxiliary materials for preparing capsules such as 180 grams of starch, mix well, and pack into capsules to make 1000 tablets.

[0016] The following pharmacodynamic experiments will further illustrate its drug activity.

[0017] Compound ChukrasoneA detects the inhibitory activity to MAO-A and MAO-B with the method of fluorescent probe, and described method is carried out according to the following steps:

[0018] Dissolve the sample to be tested in DMSO to prepare a series of samples with concentration gradient. Take 4ul of MAO (10mg / ml), boric acid buffer (PH=8.4), 50ul of BSA (50mg / ml), add the sample solution to be tested, mix well, react in a water bath at 30-38°C for 3h, then add probe 7- (3-Aminopropoxy)coumarin 2ul (50mmol / ml), inhibitor final concentration 0~10 -2 mmol / l, the mixture was then r...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to an application of Chukrasone A in preparing MAO (Monoamine Oxidase) inhibitor medicines. Compared with existing MAO inhibitors, the MAO inhibitor provided by the invention is greatly improved in inhibitory activity and selectivity to MAO-A and MAO-B. The use of the Chukrasone A for preparing MAO inhibitor medicines provided by the invention is disclosed for the first time. As the framework type belongs to a brand-new framework type, and the inhibitory activity of the Chukrasone A to MAO is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Chukrasone A has remarkable substantial characteristics and meanwhile has remarkable progress for treating diseases associated to MAO disorder.

Description

(1) Technical field [0001] The invention relates to the application of Chukrasone A in the preparation of monoamine oxidase (MAO) inhibitors. (2) Background technology [0002] Since the anti-tuberculosis drug isoniazid was found to be a potential MAO inhibitor, research on MAO inhibitors has become a hot topic. Iproniazid became the first MAO inhibitor, because it was discovered that this kind of MAO inhibitor containing hydrazine structure can also inactivate P450s and cause liver toxicity; and studied the non-hydrazine MAO inhibition represented by tranylcypromine Agents, this category can be called the second generation. But because "cheesereaction" causes 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 ChukrasoneA involved in the present invention is a new skeleton compound published in 2012 (Liu, H.B.etal., 2012.ChukrasonesAandB: Pote...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/585A61P43/00
Inventor 丁圣雨
Owner 重庆西南制药二厂有限责任公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com