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Pyrazoline aminopeptidase N inhibitors as well as preparation method and application thereof

A technology of aminopeptidase and pyrazoline, which is applied in anti-inflammatory agents, antiviral agents, and pharmaceutical formulations, and can solve the problems of limited sources, poor selectivity, unfavorable scientific research, and large-scale production

Active Publication Date: 2018-03-23
SHANDONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It is isolated from the culture fluid of Streptomyces olivorecticuli, and its total synthesis is expensive, so the source is limited
Most of the APN inhibitors that have been reported now are peptides or peptide analogs, which are sensitive to the degradation of enzymes in vivo. Due to the existence of various aminopeptidases, carboxypeptidases or dipeptidases in the body, the selectivity is poor and it is difficult to Developed into an aminopeptidase N inhibitor with clinical application value
In addition, peptide inhibitors are difficult to synthesize because they contain multiple chiral centers, and most of them are derived from natural products. The limited sources are not conducive to in-depth scientific research and large-scale production in the future

Method used

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  • Pyrazoline aminopeptidase N inhibitors as well as preparation method and application thereof
  • Pyrazoline aminopeptidase N inhibitors as well as preparation method and application thereof
  • Pyrazoline aminopeptidase N inhibitors as well as preparation method and application thereof

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Embodiment Construction

[0104] The terms and definitions used in this document have the following meanings:

[0105] "Pharmaceutically acceptable salt" refers to a therapeutically effective and non-toxic salt form of a compound of formula (I) or (II). Many such salts are known in the art. A cationic salt formed on any acidic group such as carboxyl, or an anionic salt formed on any basic group such as amino. Many such salts are known in the art, such as cationic salts including alkali metal (such as sodium and potassium) and alkaline earth metal (such as magnesium and calcium) salts and organic salts (such as amine salts). Anionic salts can also be obtained by using the corresponding acids, such acids include mineral acids such as sulfuric acid, nitric acid, phosphoric acid, hydrochloric acid, etc.; or organic acids such as acetic acid, propionic acid, glycolic acid, 2-hydroxypropionic acid, 2-oxopropionic acid Acid, oxalic acid, malonic acid, succinic acid, maleic acid, fumaric acid, malic acid, ta...

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Abstract

The invention discloses pyrazoline aminopeptidase N inhibitors as well as a preparation method and application thereof. The compounds provided by the invention have structures shown in a general formula (I) or a general formula (II). The invention also provides a preparation method of the pyrazoline compounds, and application of the pyrazoline compounds in preparation of medicines for preventing or treating diseases associated with abnormal aminopeptidase activity. The general formula (I) and the general formula (II) are shown in the description.

Description

technical field [0001] The invention relates to a pyrazoline aminopeptidase N inhibitor, a preparation method and application thereof, and belongs to the technical field of organic compound synthesis and medical application. Background technique [0002] Aminopeptidase N (APN, CD13) is a type II membrane-bound glycoprotein with a molecular weight of about 150Kd, belonging to the Gluzincins subfamily of the zinc ion-dependent metalloprotease and aminopeptidase M1 family, and exists in the form of homodimers In the cell membrane, it participates in the degradation of the N-terminal amino acid of the substrate. Studies have shown that aminopeptidase N plays an important role in tumor occurrence, development, invasion and metastasis, apoptosis and tumor angiogenesis. [0003] (1) Aminopeptidase N is highly expressed on the surface of tumor cells. The enzyme can degrade the extracellular matrix, thereby promoting the invasion and metastasis of tumor cells. The extracellular ma...

Claims

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Application Information

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IPC IPC(8): C07D231/06A61K31/415A61P35/00A61P35/02A61P29/00A61P25/00A61P1/02A61P33/06A61P31/22
CPCC07D231/06Y02A50/30
Inventor 张颖杰曹江营
Owner SHANDONG UNIV
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