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Application of 3-site functionalized N(O,S)-heterozygous indene derivative in preparation of anti-Zikavirus drug and pharmaceutical composition

A functionalized, Zika virus technology, applied in the direction of drug combination, antineoplastic drugs, and resistance to vector-borne diseases, etc.

Active Publication Date: 2020-04-07
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although a variety of anti-Zika drugs have been developed and designed based on the understanding of the life cycle of Zika virus and the interaction between Zika virus and host cells, so far there are no related vaccines or antiviral drugs approved for use. Prevention and treatment of Zika virus infection

Method used

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  • Application of 3-site functionalized N(O,S)-heterozygous indene derivative in preparation of anti-Zikavirus drug and pharmaceutical composition
  • Application of 3-site functionalized N(O,S)-heterozygous indene derivative in preparation of anti-Zikavirus drug and pharmaceutical composition
  • Application of 3-site functionalized N(O,S)-heterozygous indene derivative in preparation of anti-Zikavirus drug and pharmaceutical composition

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Experimental program
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Embodiment 1

[0035] The experimental methods described in the following examples, unless otherwise specified, are conventional methods; the reagents and biological materials, unless otherwise specified, can be obtained from commercial sources.

[0036] According to the method described in the patent (publication number CN108276323A) to prepare 3-position functionalized N(O, S)-heteroindenyl derivatives, the overall reaction process is as follows:

[0037]

[0038] where the R 1 is -H or 6-chloro, the R 2For -H, 4,6-dichloro, 5-chloro, 4-chloro, 3,4-dichloro, 2-methoxy, 4-ethoxy, 4-bromo, 3-bromo, 2-iodo, 4-fluoro, 4-tert-butyl, 4-methoxy, 3-chloro, 4-ethylphenyl, 6-ethylphenyl; the R 3 is a hydrogen atom or a methyl group.

[0039] Among them, the conditions represented by a include ethyl bromoacetate, triethylamine, dichloromethane, 0°C, 1~2h; the conditions represented by b include sodium thiosulfate pentahydrate, methanol / water=3:1(v / v), 65°C, 2h; c represents conditions includi...

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Abstract

The invention, which relates to the technical field of drug application, provides application of a 3-site functionalized N(O,S)-heterozygous indene derivative in preparation of an anti-Zikavirus drugand a pharmaceutical composition. The 3-site functionalized N(O,S)-heterozygous indene derivative has a clear Zikavirus resisting effect and has obvious inhibitory activity on replication of Zikavirus. The preliminary toxicity research shows that the derivative has high druggability and thus the derivative has the broad application prospects as an antiviral drug.

Description

technical field [0001] The invention relates to the technical field of drug application, in particular to the application and pharmaceutical composition of 3-position functionalized N(O,S)-heteroindenyl derivatives in the preparation of anti-Zika virus drugs. Background technique [0002] Zika virus (Zikavirus, ZIKV) was first isolated in 1947 from the serum of monkeys in the Zika Forest of the Victoria River in Uganda. It belongs to the flavivirus genus transmitted by mosquitoes. 11kb, encoding an open reading frame (openreading frame, ORF), which can form a polyprotein. ZIKV infection can cause outbreaks of acute infectious diseases, mainly transmitted by Aedes aegypti mosquitoes. The first recorded case of human infection with Zika virus was in 1952. After a person is infected with Zika virus, the main clinical manifestations are rash, fever, muscle pain, non-suppurative conjunctivitis, and headache. In addition, after the outbreak of the Zika epidemic, more and more e...

Claims

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Application Information

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IPC IPC(8): A61K31/404A61K31/437A61P35/00
CPCA61K31/404A61K31/437A61P35/00Y02A50/30
Inventor 张国宁王玉成王菊仙岑山朱梅王明华杜潇楠单淇牛伟萍窦月周惠宇胡尚玖
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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