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A kind of purine alkaloid and its application as anti-rsv virus drug

A technology of alkaloids and purines, applied in the field of natural medicinal chemistry, can solve the problem of no vaccine, etc., and achieve the effect of simple separation and purification method and strong inhibitory activity

Active Publication Date: 2019-05-10
深圳探影生物科技有限公司 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is currently no clinically applicable vaccine, and ribavirin (ribavirin) is the only chemotherapeutic drug used clinically (J.Med.Chem.2008,51,875–896)

Method used

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  • A kind of purine alkaloid and its application as anti-rsv virus drug
  • A kind of purine alkaloid and its application as anti-rsv virus drug
  • A kind of purine alkaloid and its application as anti-rsv virus drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] (1) Pulverization: take the whole plant of Forsythia baicalensis Scutellaria baicalensis (3kg), and after 5 days in the dark and shade, pulverize into 20-100 mesh to obtain fine powder for subsequent use;

[0020] (2) Extraction: The fine powder obtained in step (1) is ultrasonically extracted twice with ethanol with a volume fraction of 95%, each time for 20-40min, the combined extracts are freeze-dried to obtain an ethanol extract, and the ethanol extract is suspended in an appropriate amount of In the water (3L), it was extracted twice with petroleum ether (3L) and ethyl acetate (3L) successively, and the petroleum ether phase and ethyl acetate phase were combined and concentrated respectively to obtain the petroleum ether extract and the ethyl acetate extract. Ointment, spare;

[0021] (3) Purification: take the ethyl acetate part extract obtained in step (2), and first carry out normal phase silica gel column chromatography separation, stationary phase: 200-300 mes...

Embodiment 2

[0028] Antiviral activity of purine alkaloids with formula I structure of the present invention

[0029] The inhibitory activity of the purine alkaloid of formula I structure of the present invention to respiratory syncytial virus (RSV) is according to literature: Zhang, Y.J.; Stein, D.A.; Fan, S.M.; Wang, K.Y.; Kroeker, A.D.; Meng, X.J.; ; Matson, D.O.Vet.Microbiol.2006, 117(2-4), 117-129 or Grassauer, A.; Weinmuellner, R.; Meier, C.; Pretsch, A.; Prieschl-Grassauer, E.; Unger, H., Virol.J.2008,5,107. The method recorded in the test, or can be tested according to the method reported in other similar documents in the prior art.

[0030] The results show that the purine alkaloids of formula I structure have significant inhibitory effect on RSV, and its half effective concentration (EC 50 ) is less than 1μM, and the half toxic concentration (TC 50 ) greater than 100 μM, inhibition index (TI) = TC 50 / EC 50 greater than 100, while the half effective concentration (EC) of the ...

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PUM

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Abstract

The invention relates to a purine alkaloid and application thereof serving as an anti-RSV (Respiratory Syncytial Virus) drug and in particular relates to a purine alkaloid, stereisomers, tautomers or pharmaceutically acceptable salts thereof. The purine alkaloid is characterized by having a structure shown as a formula I, wherein the formula I is as shown in the specification.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, and in particular relates to a purine alkaloid and its application as an anti-RSV drug. Background technique [0002] Respiratory syncytial virus (respiratory syncytial virus, referred to as syncytial virus, RSV, also belongs to Paramyxoviridae), is an RNA virus, which belongs to Paramyxoviridae. RSV infection can cause pneumonia and a variety of lower respiratory diseases. Every year, at least 3 million infants and young children worldwide are hospitalized due to RSV virus infection, and at least 160,000 of them die. Therefore, RSV is also known as a child killer (Science, 2013, 342, 546 -547). Currently there is no clinically applicable vaccine, and ribavirin (ribavirin) is the only chemotherapeutic drug used clinically (J.Med.Chem.2008, 51, 875-896). In summary, it is urgent to develop drugs for preventing and / or treating diseases caused by RSV infection. Contents of the inventio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D473/30A61K31/522A61P31/14
CPCC07D473/30
Inventor 郑超张宏李音
Owner 深圳探影生物科技有限公司
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