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A compound for promoting Aβ aggregation and its preparation method and application

A compound and reaction technology, applied in the field of compounds that promote Aβ aggregation and their preparation, can solve problems such as poor effect and nerve cell death

Active Publication Date: 2017-05-24
BEIJING NORMAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Early views believed that fibrous Aβ was neurotoxic and was the main cause of neuronal cell death and ultimately AD (1.Lorenzo and Yankner, 1996A.Lorenzo, B.A.YanknerAmyloid fibril toxicity in Alzheimer's disease and diabetes Ann.NY Acad. Sci., 77(1996), pp.89–95; 2. Liu, Y. (1999), "Understanding the biological activity of amyloid proteins in vitro: from inhibited cellular MTT reduction to altered cellular cholesterol homeostatis", Progress in Neuro‐psychopharmacology & Biological Psychiatry, Vol.23, pp.377‐95.), so inhibiting Aβ aggregation is one of the important targets of drug screening for a long time, but the progress of related research is very little, and the screened drugs enter clinical trials not effectively

Method used

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  • A compound for promoting Aβ aggregation and its preparation method and application
  • A compound for promoting Aβ aggregation and its preparation method and application
  • A compound for promoting Aβ aggregation and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0038] Embodiment 1, compound shown in preparation formula I

[0039] Using hydrochloric acid as a catalyst, the compound represented by formula II was deprotected in 62% ethanol aqueous solution for 2 hours. After the reaction was completed, 0.0516 g of the compound represented by formula I provided by the present invention was obtained as a brown yellow solid.

[0040]

[0041] of the compound 1 H-NMR and 13 C-NMR detection results are as follows: 1 H NMR (500MHz, DMSO-d 6 )δ9.51(s,1H),8.69(s,1H),6.89(dd,J=7.8,1.3Hz,1H),6.79(dd,J=7.8,1.3Hz,1H),6.69(t,J =7.8Hz,1H),6.22(d,J=2.3Hz,1H),6.20(d,J=2.3Hz,1H),5.67(dd,J=12.7,2.8Hz,1H),3.81(s,3H ),3.78(s,3H),2.95(dd,J=16.3,12.7Hz,1H),2.59(dd,J=16.3,2.8Hz,1H).

[0042] 13 C NMR (126MHz, DMSO-d 6 )δ188.21, 165.37, 164.67, 161.80, 145.15, 142.43, 125.88, 119.05, 116.87, 115.06, 105.31, 93.66, 92.82, 73.94, 55.87, 55.72, 43.81.

[0043] It can be seen from the above that the compound has a correct structure and is the target com...

Embodiment 2

[0044] The activity evaluation experiment of the compound shown in embodiment 2, embodiment 1 gained formula I:

[0045] 1. Aβ monomerization treatment

[0046] AmyloidβPeptide (1-42) (human) freeze-dried powder was purchased from Abcam. Take out 1 mg of Aβ1-42 dry powder from the -20°C refrigerator, and add 1 ml of HFIP (1,1,1,3,3,3-hexafluoro-2-propanol) (Fluka) to a final concentration of 1 mg / ml. Incubate at room temperature for 1 h, vortex at medium speed from time to time to mix. Then the Aβ solution was sonicated in a water bath for 10 minutes to completely monomerize Aβ1-42. After ultrasonication, the solution was centrifuged at 13,000 g for 20 min, and the solution was divided into 1.5 ml EP tubes. After sealing with parafilm, a few small holes were pierced with a syringe needle, and the centrifuge tubes were placed in a fume hood to completely volatilize the HFIP and then stored at -80°C. The monomerized Aβ was resuspended in DMSO to a stock solution concentration...

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Abstract

The invention discloses a compound for promoting Abelta gathering and a preparation method and application thereof. The structural formula of the small molecule compound for promoting Abelta gathering is shown in the formula I. Under the condition that acid serves as a catalyst, a deprotection reaction is conducted on a compound shown in the formula II in ethanol water, and the compound for promoting Abelta gathering is obtained through reaction. According to the compound shown in the formula I, the concentration of oligomers with high toxicity can be reduced by accelerating Abelta to gather to polymers with lower toxicity from monomers, and therefore the purpose of treating is achieved. (The formula I and the formula II are shown in the specification).

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a compound for promoting Aβ aggregation, its preparation method and application. Background technique [0002] Alzheimer's disease (AD) is a kind of neurodegenerative disease. Its early symptoms usually manifest as loss of short-term memory, and then develop into memory confusion, aphasia, irritability, and cognitive dysfunction. The most common type of dementia. . There are more than 6 million senile dementia patients in my country, accounting for about a quarter of the total number of patients in the world. It is predicted that with the increase of population aging, there will be more than 100 million Alzheimer's patients in the world by the middle of this century. [0003] Senile plaques (SP) formed by the accumulation of amyloid-beta (Aβ) outside nerve cells are one of the two important pathological features of Alzheimer's disease. Aβ is formed by cleavage of its precursor protein AP...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/32A61K31/352A61P25/28A61P43/00
CPCC07D311/32
Inventor 赵长琦张辰窦非
Owner BEIJING NORMAL UNIVERSITY
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