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Application of pyrilamine compounds to preparation of acetylcholinesterase inhibitor

A technology of acetylcholinesterase and pyrimidine amines, which is applied in the field of pyrimidine amine compounds and can solve the problems that there are no pyrimidine amine compounds

Inactive Publication Date: 2012-09-12
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Acetylcholinesterase plays an important role in the transmission of nerve impulses in the body. It is a choline ester hydrolase and belongs to a completely different target category from tyrosine kinase receptors such as VEGFR2. There is no pyrimidine amine in the prior art. Related reports of compounds used as acetylcholinesterase inhibitors

Method used

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  • Application of pyrilamine compounds to preparation of acetylcholinesterase inhibitor
  • Application of pyrilamine compounds to preparation of acetylcholinesterase inhibitor
  • Application of pyrilamine compounds to preparation of acetylcholinesterase inhibitor

Examples

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preparation example Construction

[0039]The preparation of the acetylcholinesterase inhibitor of the present invention includes combining the compound of formula I described in the present invention, or its pharmaceutically acceptable salt and solvate thereof, with a common pharmaceutical adjuvant or carrier to prepare a compound having acetylcholinesterase Pharmaceutical compositions with enzyme inhibitory activity. The above-mentioned pharmaceutical composition can adopt dosage forms such as tablets, granules, capsules, oral liquids, injections, and aerosols; it can also adopt controlled-release or sustained-release dosage forms or nano-preparations known in the modern pharmaceutical industry. Regarding the selection of preparation methods and methods, it is believed that those skilled in the art can obtain sufficient facts from the prior art, and the present invention will not repeat them.

[0040] Following non-restrictive embodiment can make those of ordinary skill in the art understand the present invent...

Embodiment

[0042] Pazopanib (compound 1) inhibits acetylcholinesterase activity detection

[0043] The pyrimidine amine compound pazopanib (compound 1) used in the test of the present invention was prepared according to the method reported in the literature: US 2009 / 0005406A1 (disclosure date: January 1, 2009).

[0044]

[0045] Inhibition of acetylcholinesterase activity detection test:

[0046] Fresh acetylcholinesterase, purchased from Sigma company;

[0047] Thioacetylcholine salt (ATOH) was purchased from Sigma as a substrate;

[0048] 5,5-dithiobis(2-nitrobenzoic acid) (DTNB) is a chromogen, purchased from Sigma;

[0049] 0.01M phosphate buffer (pH=7.0);

[0050] Pazopanib was made into DMSO solution (both 20 μmol / mL).

[0051] Detection method:

[0052] (1) Acetylcholinesterase and substrate are prepared with 0.01M phosphate buffer solution at a suitable concentration. 1ml of the initial reaction system contains 0.02 units of enzyme, 0.1 μmol of substrate, 0.1 μmol of chro...

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Abstract

The invention relates to application of pyrilamine compounds to the preparation of an acetylcholinesterase inhibitor. The pyrilamine compounds have a structure of a general formula I, wherein in the general formula I, S1 is selected from O, S, -CH2- and -NH-; S2 is selected from O, S, -N(CH3)-, -NH- and -(CH2)n-, and n is an integral number of 1 to 6; Q1 is selected from hydrogen, halogens, straight chain or branched chain alkyl, cycloalkyl, trihaloalkyl and alkoxy; Q2 and Q3 are selected from the hydrogen, the halogens, the straight chain or branched chain alkyl, the cycloalkyl, the trihaloalkyl, the alkoxy, aryl, heteroaryl, -(CO)R1 and -S(O2)R2 independently and respectively; R1 and R2 are selected from straight chain or branched chain alkyl having 1 to 4 carbon atoms and amino independently and respectively; and X1 and X2 are respectively selected from H, the straight chain or branched chain alkyl having 1 to 4 carbon atoms and haloalkyl having 1 to 4 carbon atoms independently.

Description

technical field [0001] The invention relates to a new application of a class of pyrimidine amine compounds. Background technique [0002] Acetylcholine (Ach) is a neurotransmitter that mainly exists in the presynaptic cholinergic nerve endings. In the brain, maintaining a certain level of acetylcholine plays an important role in human memory and recognition functions; in the motor nervous system, acetylcholine exists at the neuromuscular junction and controls muscle contraction; in the sympathetic nerve, acetylcholine is released by the preganglionic nerve Neurotransmitters play an important role in maintaining normal physiological functions in the body. Acetylcholinesterase (AchE) mainly exists in the neuromuscular junction and cholinergic nervous system, and its physiological function in the body is to hydrolyze and inactivate acetylcholine. Acetylcholinease inhibitors can block the activity of AchE, delay the hydrolysis rate of acetylcholine, increase the level of acety...

Claims

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Application Information

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IPC IPC(8): A61K31/506C07D403/12A61P21/04A61P25/28A61P27/06
Inventor 杨永亮牛铭山
Owner DALIAN UNIV OF TECH
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