Application of dihydroartemisinin and quinolone conjugate in preparation of drugs for resisting leishmania

A quinolone conjugate, dihydroartemisinin technology, applied in the direction of anti-infective drugs, drug combinations, resistance to vector-borne diseases, etc., can solve the safety and toxicity problems of leishmaniasis, lack of compliance, and drug resistance and other issues to achieve the effect of broadening the use of pharmaceuticals

Active Publication Date: 2019-10-25
SOUTHWEST UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Current treatments for leishmaniasis have safety/toxicity issues (including cardiotoxicity), incomplete cure rate

Method used

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  • Application of dihydroartemisinin and quinolone conjugate in preparation of drugs for resisting leishmania
  • Application of dihydroartemisinin and quinolone conjugate in preparation of drugs for resisting leishmania
  • Application of dihydroartemisinin and quinolone conjugate in preparation of drugs for resisting leishmania

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1. Preparation of target compound

[0036] 1. Synthesis of the target compound TM1 series

[0037] 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).

[0038]

[0039]

[0040] 2. Synthesis of the target compound TM9 series

[0041] 1) Synthesis of intermediate IM3

[0042] 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).

[0043] 2) Synthesis of target compound TM9 series

[0044]

[0045] 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 ...

Embodiment 2

[0078] Example 2. Anti-Leishmania activity test of target compound

[0079] The anti-Leishmania activity of the target compound was tested by the Open Innovation Drug Discovery (OIDD) program of Eli Lilly and Company in the United States. First, a single-concentration primary screening (Primary SP) was carried out, and then a multi-concentration test (Primary CRC ). The test results of anti-Leishmania activity of some compounds are shown in Table 3.

[0080] Anti-Leishmania activity test results of some compounds in table 3

[0081]

[0082] The Primary SP test results in Table 3 show that the target compounds TM1, TM9, TM10, and TM11-1 can all inhibit the growth of Leishmania donovani (L.donovani), wherein TM9-1, TM9-2, TM9-3, and TM9 -5 The growth inhibition rate of Leishmania donovani at 5 μM test concentration is close to or exceeds 95%; Primary CRC test results show that the pIC of the target compounds TM1, TM9 and TM10 on the growth of Leishmania donovani 50 (Negat...

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PUM

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Abstract

The invention discloses application of a dihydroartemisinin and quinolone conjugate shown in a formula I in preparation of drugs for resisting leishmania. The pharmaceutical application of the dihydroartemisinin and quinolone conjugate is broadened.

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 anti-Leishmania medicaments. 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): A61K31/357A61K31/4709A61K31/496A61P33/02
CPCA61K31/357A61K31/4709A61K31/496A61P33/02A61K2300/00Y02A50/30
Inventor 杨大成孙晓丽罗鹏唐雪梅范莉周福委李洋
Owner SOUTHWEST UNIVERSITY
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