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A class of conjugates of triterpenes and straight-chain amino derivatives and their applications

A straight-chain amino and derivative technology, applied in the directions of medical preparations containing active ingredients, steroids, organic chemistry, etc., can solve the problem that the inhibitory effect of influenza virus has not been reported, and achieves enhanced anti-influenza virus activity, enhanced Biocompatible, fast and efficient response

Active Publication Date: 2021-07-16
KUNMING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inhibitory effect of the conjugates of triterpenes and linear amino derivatives on influenza virus has not been reported.

Method used

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  • A class of conjugates of triterpenes and straight-chain amino derivatives and their applications
  • A class of conjugates of triterpenes and straight-chain amino derivatives and their applications
  • A class of conjugates of triterpenes and straight-chain amino derivatives and their applications

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1: The preparation method of the conjugate of this triterpene and straight-chain amino derivatives can be prepared by the following technical routes:

[0060]

[0061] Wherein, compound M22 is synthesized as follows:

[0062]

[0063] Get 1g of oleanolic acid (OA) in a 50mL reaction bottle, dissolve it in 20mL DMF, add 845mg TBTU and 340mgDIEA, react at room temperature, TLC detection after 12h, developer ratio petroleum ether: ethyl acetate=3:1; Completely evaporate DMF to dryness, use water / ethyl acetate system (water:ethyl acetate volume ratio 1:1) to extract 3 times, take the organic phase in MgSO 4 After drying, the solvent was evaporated and recrystallized (ethanol:water=3:1); 1582 mg of white flocculent solid M38 was obtained with a yield of 92.8%, which was ready for use;

[0064] Take 1g of compound M38 in a 50mL reaction flask, dissolve in 15mL of DMF, add 217mg of 4-aminobutanol, then add 1.2eq of sodium carbonate, react at room temperature,...

Embodiment 2

[0095] Embodiment 2: The compound of the present invention inhibits the biological activity evaluation method of influenza virus entering cells

[0096] 1. Cytopathic Efficacy (CPE) Inhibition Test

[0097] After influenza virus infects cells, it will cause cell pathology, which will reduce cell viability; if the drug can inhibit the replication of influenza virus, it will reduce the number of cell lesions and increase cell viability; specifically:

[0098] (1) Canine kidney epithelial cells (MDCK) were passaged into a white 96-well plate at a ratio of 1:3, and cultured in DMEM medium containing 10% FBS for 24 hours in a cell culture incubator at 37°C;

[0099] (2) Add influenza virus [A / WSN / 33 (H1N1), multiplicity of infection (MOI) = 1] and 100 μM / L of the compound to be tested to 100 μl of DMEM containing 2 μg / mL TPCK-treated trypsin and 1% FBS Mix well; the negative control of the compound is 1% DMSO (the solvent used for diluting the compound); set up a group of experime...

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PUM

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Abstract

The present disclosure discloses a conjugate of a triterpene and a straight-chain amino derivative whose structural formula is as follows: the compound is used in the preparation of a medicine for treating or / or preventing influenza, and the experimental results show that the triterpene and the straight-chain amino derivative The conjugate has obvious inhibitory effect on influenza virus, and can significantly inhibit influenza virus from entering cells; the compound in the present invention targets at the stage of influenza virus entering cells, inhibits influenza virus infection from the source, and is an anti-influenza virus inhibition Drug research provides a basis.

Description

technical field [0001] The invention relates to a conjugate of a triterpene and a linear amino derivative and an application thereof. Background technique [0002] Influenza is an acute, contagious respiratory disease caused by influenza virus. According to the antigenicity of its internal nucleoprotein (NP) and matrix protein (M), influenza virus can be divided into A type, B type, C type and D type. The large-scale epidemic of type A (also known as type A) influenza virus can cause extremely high morbidity and mortality, which seriously threatens human health (Virology Journal. 2007, 4, 1-5). Influenza A virus mainly caused three major influenzas in the 20th century, namely H1N1 in 1918, H2N2 in 1957 and H3N2 in 1968, causing a total of about 50 million deaths (Emerging Infectious Diseases. 2006, 12, 9-14; Journal of the American Medical Association, 2007, 18, 2025-2027). Influenza A in 2009 was also caused by H1N1 influenza virus (New England Journal of Medicine. 2009,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P31/16
CPCA61P31/16C07J63/008
Inventor 俞飞孟令宽杨帆苏扬清李唯嘉邵亮周德敏
Owner KUNMING UNIV OF SCI & TECH
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