Anti-AIDS compound, its preparing method and pharmaceutical composition with anti-AIDS compound as active component and use thereof

A kind of technology of compound and medicine, applied in the field of application in the preparation of anti-AIDS medicine

Inactive Publication Date: 2005-07-06
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, in the prior art, there is no report on the novel structure of the compound of formula I of the present invention, the high oxidation degree new skeleton nortriterpenoid Schizandrin B, C and its analogues, and there is no such compound as an active ingredient in the treatment of disease reports

Method used

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  • Anti-AIDS compound, its preparing method and pharmaceutical composition with anti-AIDS compound as active component and use thereof
  • Anti-AIDS compound, its preparing method and pharmaceutical composition with anti-AIDS compound as active component and use thereof
  • Anti-AIDS compound, its preparing method and pharmaceutical composition with anti-AIDS compound as active component and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Schizandrin B(1) (1,4-epoxy-9β,14α,15β,22α-tetrahydroxy-3,4:9,10-seco-28-nor-cycloartane-24-en-1,3:23 , 26-diolide, 1) (hereinafter referred to as the preparation of compound 1):

[0035] Dried Schisandra micrantha A.C.Smith stems and leaves 6.8kg, crushed, soaked in acetone aqueous solution at room temperature for 3 times (about 25 liters each time), combined the extracts, distilled off the acetone under reduced pressure, let stand overnight, and filtered out the sediment The pigment, the filtrate was first extracted 2 times with petroleum ether, and then extracted 3 times with ethyl acetate. After recovering the solvent, the ethyl acetate part (170g) was obtained. The ethyl acetate part was mixed with 300g of crude silica gel (80-100 mesh), and 1.4kg of silica gel (100-200 mesh) was roughly separated on a thick and short silica gel column, and washed with a gradient of chloroform:acetone (1:0→6:4) Each 1000ml is a fraction, a total of 300 parts. TLC Monitoring Ident...

Embodiment 2

[0082] Schisandrin C(2)

[0083] (1, 4:14, 15-diepoxy-9β, 22α-dihydroxy-3, 4:9, 10-seco-28-nor-cyclartane-24-en-1, 3:23, 26-diolide, 2)( Hereinafter referred to as compound 2) preparation:

[0084] Dried Schisandra micrantha A.C.Smith stems and leaves 6.8kg, crushed, soaked in acetone aqueous solution at room temperature for 3 times (about 25 liters each time), combined the extracts, distilled off the acetone under reduced pressure, let stand overnight, and filtered out the sediment The pigment, the filtrate was extracted 3 times with ethyl acetate, after recovering the solvent, the ethyl acetate part (170g) was obtained. The ethyl acetate part was mixed with 300 g of crude silica gel (80-100 mesh), and 1.4 kg of silica gel (100-200 mesh) was roughly separated on a thick and short silica gel column, and washed with a gradient of chloroform: acetone (1:0 → 6:4). Each 1000ml is a fraction, a total of 300 parts. TLC Monitoring Identical fractions were pooled to give 8 major fr...

Embodiment 3

[0093] Using Example 1 or 2 as an active natural lead compound, carry out structural modification to obtain other derivatives represented by formula (1) as active ingredients of the medicine of the present invention.

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PUM

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Abstract

Provided are a compound of the formula (1), preparing method thereof, a pharmaceutical composition using the compound as active constituent, wherein a schisandra fruit lactone of compound of the formula (1) containing effective dose for the treatment of AIDS and a medicinal carrier and / or an excipient are included, and their uses in AIDS treatment medicine and reverse transcriptase inhibitor medicine.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and in particular, relates to a class of anti-AIDS compounds Schizandrin B, C and their analogs, their preparation methods, pharmaceutical compositions with such compounds as active ingredients and their preparation in reverse transcription Application of enzyme inhibitor drug neutralization in the preparation of anti-AIDS drugs. technical background: [0002] Since the first AIDS (Acquired Immunodeficiency Syndrome, AIDS) report in 1981, its epidemic has spread rapidly to countries all over the world. At present, more than 60 million people have been infected and more than 20 million people have died, causing immeasurable economic and social losses. AIDS in my country has entered a period of rapid development since 1995, with an annual growth rate of 30%. According to the latest data released by the Ministry of Health, the cumulative number of HIV-infected people in mainland my country has e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P31/18C07D493/04
Inventor 李蓉涛孙汉董郑永唐王睿睿杨柳萌林中文赵勤实
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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