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Use of dipeptide analogue

A technology of use and medicine, applied in the field of medicinal chemistry, can solve the problems of high mortality, no medicine for dengue virus, no vaccine, etc.

Active Publication Date: 2014-02-19
NANJING TECH UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Under the influence of many factors such as the deterioration of the global environment and warming, the dengue fever epidemic has been expanding in recent years, but there is currently no effective vaccine for preventing the occurrence and prevalence of dengue fever, and there is no effective anti-dengue virus drug available for clinical treatment For dengue fever, the current clinical treatment is mainly intensive supportive therapy, in which maintaining fluid balance is the main means
These limited means cannot cope with the high mortality rate (~5%) of DHF and DSS caused by dengue virus infection, so the drug research on dengue fever disease caused by dengue virus infection is extremely important and urgent

Method used

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Embodiment 1

[0027]The constructed NS3-NS2B fusion protein expression plasmid PET15b-CF40-Linker-NS3pro185 (CF40 is the 40 amino acids in the core sequence of the hydrophilic region of NS2B between 1394-1440, Linker is the sequence that Gly4-Ser-Gly4 can rotate freely, NS3pro185 It is the 185 amino acid sequence between 1476-1660 of the N-terminal of NS3) provided by Dr. Siew Phengsuozeg Lim, Novartis Institute of Tropical Diseases, Singapore (see Jun Li, Siew Pheng Lim, David Beer, Viral Patel, Daying Wen, Christine Tumanut, David C. Tully, Jennifer A. Williams, Jan Jiricek, John P. Priestle, Jennifer L. Harris, and Subhash G. Vasudevan J. Biol. Chem. 2005, 280(31), 28766-28774.). NS3-NS2B fusion protein expression plasmid PET15b-CF40-Gly-NS3pro185 in Escherichia coli BL21 (DE3) The recombinantly expressed protease can be used through the histidine tag (His-tag) and Ni 2＋ The affinity chromatography column is supplemented with other chromatographic methods for purification, and the purifi...

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Abstract

The invention discloses use of a dipeptide analogue, and particularly relates to use of compounds in formulas (I) and (II), a stereisomer or a pharmaceutically acceptable salt thereof in pharmaceutical aspects. The compounds shown in the formulas (I) and (II) can be utilized as drugs for treating and preventing a disease caused by a dengue fever virus, and simultaneously can become the drugs for treating and preventing the disease caused by other flaviviruses, such as a yellow fever disease, hepatitis c, Japanese encephalitis, forest encephalitis, a disease caused by west nile virus infection, or aids caused by a human immunodeficiency virus (HIV) and the like.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to the application of dipeptide analog compounds, stereoisomers, or pharmaceutically acceptable salts thereof in pharmacy. Background technique [0002] The compound of formula (I) has been used as the substrate of methionine aminopeptidase for drug screening of angiogenesis (Ying Zhou, Xiao-Chuan Guo, Tian Yi, Tadashi Yoshimoto, Dehua Pei Analytical Biochemistry 2000, 280, 159-165. ) [0003] [0004] And formula (II) is the raw material of formula (I) (Ying Zhou, Xiao-Chuan Guo, Tian Yi, Tadashi Yoshimoto, Dehua Pei Analytical Biochemistry 2000, 280, 159–165.) [0005] [0006] Dengue fever disease includes dengue fever (dengue fever, DF), dengue hemorrhagic fever (dengue hemorrhagic fever, DHF) and dengue shock syndrome (dengue shock syndrome, DSS) symptoms, it is caused by the flaviviridae dengue virus (dengue virus, DENV) infection. Dengue fever is mainly ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61P31/14A61P31/18
CPCY02A50/30
Inventor 周国春翁智兵王春光邵晓霞聂鑫
Owner NANJING TECH UNIV
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