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2-amino-1-(4-nitro phenyl)-1-ethanol metalloid protease inhibitor, and preparation and use thereof

A technology of nitrophenyl and amino, applied in the field of drug synthesis

Inactive Publication Date: 2009-08-12
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

5) APN participates in the degradation of endogenous analgesic substances endorphins and enkephalins, thereby causing excessive release of substance P, leading to pain

Method used

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  • 2-amino-1-(4-nitro phenyl)-1-ethanol metalloid protease inhibitor, and preparation and use thereof
  • 2-amino-1-(4-nitro phenyl)-1-ethanol metalloid protease inhibitor, and preparation and use thereof
  • 2-amino-1-(4-nitro phenyl)-1-ethanol metalloid protease inhibitor, and preparation and use thereof

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Experimental program
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Embodiment Construction

[0106] The terms and definitions used in this document have the following meanings:

[0107] "Heteroalkyl" means a saturated or unsaturated chain comprising carbon atoms and at least one heteroatom, none of which are adjacent. The heteroalkyl group contains 2-15 atoms (carbon atoms), preferably 2-10 atoms. Heteroalkyl groups can be straight or branched, substituted or unsubstituted.

[0108] "Aryl" means an aromatic carbocyclic group. Preferred aromatic rings contain 6-10 carbon atoms.

[0109] "Halo", or "halogen" includes fluorine, chlorine, bromine or iodine, preferably fluorine and chlorine.

[0110] "Cycloalkyl" is a substituted or unsubstituted, saturated or unsaturated cyclic group containing carbon atoms and / or one or more heteroatoms. The ring may be a monocyclic or fused, bridged or spiro ring system. Monocyclic rings generally contain 3-9 atoms, preferably 4-7 atoms, and polycyclic rings contain 7-17 atoms, preferably 7-13 atoms.

[0111] "Heteroaryl" is an ar...

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Abstract

The invention relates to a 2-amino-1-(4-nitrobenzophenone)-1-ethanol metalloproteinase inhibitor as well as a preparation and application thereof. The 2-amino-1-(4-nitrobenzophenone)-1-ethanol metalloproteinase inhibitor is a compound with the following general formula (1). Dipeptide-like or kyrine-type compounds of different series can enhance the appetency and metabolization stability of a compound and an enzyme or a receptor and conforms to the basic requirement on inhibitor structures. The invention designs and synthesizes a group of aminopeptidase N inhibitors with totally new structures. A vitro test shows that the inhibitors have no cytotoxin activity, and four compounds which exhibit remarkable vitro inhibitory activity are close to positive control medicine bestatin and can be used as candidate anticancer medicines. The invention also relates to a pharmaceutical composition of a peptide-like compound with a structure indicated by formula (I), and also relates to the pharmacy usage of the pharmaceutical composition.

Description

technical field [0001] The present invention relates to a class of peptidoid compound with the function of inhibiting metalloprotease, its preparation method, activity test, composition containing the peptidoid compound, and the application of these compositions. It belongs to the field of drug synthesis. Background technique [0002] 1. Aminopeptidase N [0003] 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. APN is widely expressed in kidney and intestinal brush border cells, bone marrow progenitor cell membranes, monocyte membranes, central nervous system synaptic cell membranes, fibroblasts, endothelial cell membranes, and placental cell membranes, participating...

Claims

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Application Information

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IPC IPC(8): C07C237/20C07D317/58C07D209/14C07C259/06C07C233/78C07C235/50C07C323/25C07C271/22C07C271/20C07C231/12C07K5/09A61K31/165A61K31/36A61K31/404A61K31/166A61K38/06A61P43/00A61P29/00A61P35/00A61P37/00A61P1/04A61P1/02A61P35/02
CPCY02P20/55
Inventor 徐文方杨康辉方浩
Owner SHANDONG UNIV
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