Application of dihydroartemisinin and carbostyril conjugates to preparation of medicines for reducing blood lipid

A quinolone conjugate, dihydroartemisinin technology, applied in the directions of drug combination, pharmaceutical formula, medical preparation containing active ingredients, etc., to achieve the effect of broadening the use of pharmaceuticals

Active Publication Date: 2019-11-26
SOUTHWEST UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Quinolones (such as ciprofloxacin, ofloxacin, levofloxacin, moxifloxacin, and gatifloxacin) are currently the drugs of choice for the treatment of extensively multidrug-resistant tuberculosis (MDR-TB), which are highly effective against Mycobacterium tuberculosis. Good inhibitory or killing effect, and no obvious cross-resistance with non-quinolone anti-tuberculosis drugs, no inhibitory effect on the activity of these drugs when used in combination, but long-term use of quinolone drugs will promote resistance to marketed quinolone drugs Mycobacterium tuberculosis

Method used

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  • Application of dihydroartemisinin and carbostyril conjugates to preparation of medicines for reducing blood lipid
  • Application of dihydroartemisinin and carbostyril conjugates to preparation of medicines for reducing blood lipid
  • Application of dihydroartemisinin and carbostyril conjugates to preparation of medicines for reducing blood lipid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1. Preparation of target compound

[0035] 1. Synthesis of the target compound TM1 series

[0036] The target compounds TM1 series (TM1-1~TM1-12) were prepared according to the method described in Chinese patent 104418864B (conjugates of dihydroartemisinin and quinolones and their preparation methods and applications).

[0037]

[0038] 2. Synthesis of the target compound TM9 series

[0039] 1) Synthesis of intermediate IM3

[0040] The intermediate IM3 was prepared according to the method described in Chinese patent 104418864B (conjugates of dihydroartemisinin and quinolones and its preparation method and application).

[0041] 2) Synthesis of target compound TM9 series

[0042]

[0043] Add IM3 (1mmol) and 3mL of dichloromethane (DCM) into a 100mL reaction flask, stir at -10°C to 0°C, and partially dissolve, then add N,N'-diisopropylethylamine (DIPEA, 1.5mmol) in sequence , Pivaloyl chloride (1.5mmol), -10 ℃ ~ 0 ℃ continue to stir the reaction for...

Embodiment 2

[0076] Example 2. PCSK9 inhibitory activity test of target compound

[0077] The PCSK9 inhibitory activity of the target compound was tested by Eli Lilly's Open Innovation Drug Discovery (OIDD) program. First, a single-concentration primary screening (Primary SP) was performed, and then a multi-concentration test (Primary CRC) was performed on the potential molecules screened out initially. The test results of PCSK9 inhibitory activity of some compounds are shown in Table 3 and Table 4.

[0078] Table 3PCSK9Inhibition (Eff-1) activity test result

[0079]

[0080] Table 3 tested the inhibition rate of the target compound TM1 series on the secretion of PCSK9 from human liver cancer cells HepG2 and the toxicity to HepG2 cells. The results of the Primary SP test showed that the target compound TM1 series could inhibit the secretion of PCSK9 from HepG2 cells. At a test concentration of 20 μM, the inhibition rate of 10 compounds exceeded 90%, and the inhibition rate of 6 compou...

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PUM

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Abstract

The invention discloses an application of dihydroartemisinin and carbostyril conjugates to preparation of medicines for reducing blood lipid, as shown in the formula I, and the pharmacy application iswidened.

Description

technical field [0001] The invention belongs to the technical field of medical application of compounds, and relates to the application of a class of dihydroartemisinin and quinolone conjugates in the preparation of blood lipid-lowering drugs. Background technique [0002] Dihydroartemisinin is an artemisinin derivative with high-efficiency and low-toxic antimalarial activity. Studies in recent years have shown that dihydroartemisinin and its derivatives also have various biological activities such as anti-tumor, anti-inflammation, and anti-fibrosis. [0003] Quinolones (such as ciprofloxacin, ofloxacin, levofloxacin, moxifloxacin, and gatifloxacin) are currently the drugs of choice for the treatment of extensively multidrug-resistant tuberculosis (MDR-TB), which are highly effective against Mycobacterium tuberculosis. Good inhibitory or killing effect, and no obvious cross-resistance with non-quinolone anti-tuberculosis drugs, no inhibitory effect on the activity of these ...

Claims

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Application Information

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IPC IPC(8): A61K31/4709A61K31/4375A61K31/437A61K31/496A61P3/06
CPCA61K31/4709A61K31/4375A61K31/437A61K31/496A61P3/06Y02A50/30
Inventor 杨大成范莉唐雪梅罗鹏周福委孙晓丽潘建芳
Owner SOUTHWEST UNIVERSITY
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