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Ring-fused compound of tetrahydropyrrole and piperazinedione as well as preparation and pharmaceutical application of ring-fused compound of tetrahydropyrrole and piperazinedione

A technology of diketopiperazine and tetrahydropyrrole is applied in the field of medicinal chemistry, and can solve the problems of clinical treatment of dengue fever diseases without dengue virus.

Active Publication Date: 2022-07-29
CHANGZHOU VOCATIONAL INST OF ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Under the influence of many factors such as global environmental deterioration and warming, the dengue fever epidemic has been expanding in recent years. However, there is currently only one dengue vaccine in a limited area, and there is no effective anti-dengue virus drug available for clinical treatment of dengue fever. Now clinical treatment is mainly gradual supportive therapy, in which maintaining fluid balance is the main means

Method used

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  • Ring-fused compound of tetrahydropyrrole and piperazinedione as well as preparation and pharmaceutical application of ring-fused compound of tetrahydropyrrole and piperazinedione
  • Ring-fused compound of tetrahydropyrrole and piperazinedione as well as preparation and pharmaceutical application of ring-fused compound of tetrahydropyrrole and piperazinedione
  • Ring-fused compound of tetrahydropyrrole and piperazinedione as well as preparation and pharmaceutical application of ring-fused compound of tetrahydropyrrole and piperazinedione

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Embodiment 1

[0032] The present invention provides a preparation method of the above compound, comprising the following steps:

[0033]

[0034] The following specific compounds were prepared as described above:

[0035]

[0036]

[0037]

[0038]

Embodiment 2

[0040] Protease activity assay procedures refer to published papers. (Zhou G C, Weng Z, Shao X, et al. Discovery and SAR studies of methionine-proline anilides as dengue virusNS2B-NS3 protease inhibitors[J].Bioorganic&medicinal chemistry letters,2013,23(24):6549-6554.) Partial compounds Activity data for NS2b-NS3 are presented below.

[0041]

[0042]

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PUM

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Abstract

The invention is applicable to the field of medicinal chemistry, and provides a fused ring compound of tetrahydropyrrole and piperazinedione as well as preparation and pharmaceutical application of the fused ring compound, and the compound is a compound shown in the formula or other pharmaceutically acceptable salts. The compound disclosed by the invention has the functions of inhibiting infection and replication of the dengue virus, so that the compound disclosed by the invention can be used as a medicine for preventing and treating diseases caused by the dengue virus.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a cyclic compound of tetrahydropyrrole and diketopiperazine and its preparation and pharmaceutical use. Background technique [0002] Dengue fever (DF) is an acute infectious disease caused by dengue virus (DENV), which is transmitted through the bite of female mosquitoes. Dengue hemorrhagic fever (DHF) and dengue shock syndrome (DSS). About 390 million people are infected with DENV each year, affecting 128 countries. [0003] Under the influence of many factors such as global environmental deterioration and warming, the dengue fever epidemic has tended to expand in recent years, but currently there is only one dengue vaccine for limited areas, and no effective anti-dengue virus drugs can be used for clinical treatment of dengue fever disease. The current clinical treatment is mainly progressive supportive therapy, in which the maintenance of body fluid balance is the main me...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/4985A61P31/14
CPCC07D487/04A61P31/14C07B2200/07Y02A50/30
Inventor 翁智兵周海平田苗陈绘如
Owner CHANGZHOU VOCATIONAL INST OF ENG