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Application of compound in preparation of kallikrein KLK7 inhibition medicines, and synthesis method of compound

A kallikrein and compound technology, applied in the field of biomedicine, can solve the problems of inability to penetrate the stratum corneum of the skin, slow absorption and diffusion, and fast degradation, and achieves a simple and easy synthesis method, stable inhibition effect, and inhibition efficiency. high effect

Active Publication Date: 2017-01-18
CHINA THREE GORGES UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although LEKTI is a natural inhibitor of KLK7 in the epidermis, as an external drug for the treatment of AD, it cannot penetrate the stratum corneum of the skin, and the characteristics of its macromolecular protein will also lead to the problems of slow absorption and diffusion and rapid degradation. so very limited
So far, no effective KLK7 inhibitor has been used clinically

Method used

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  • Application of compound in preparation of kallikrein KLK7 inhibition medicines, and synthesis method of compound
  • Application of compound in preparation of kallikrein KLK7 inhibition medicines, and synthesis method of compound
  • Application of compound in preparation of kallikrein KLK7 inhibition medicines, and synthesis method of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The application of the compound in the preparation of the medicine for inhibiting kallikrein KLK7, the structural formula of the compound is:

[0037]

Embodiment 2

[0039] The method for the compound described in Synthetic Example 1, the synthetic route is as follows:

[0040]

[0041] in:

[0042] Synthesis of Substance 18: Substance 17, KOH, water, and carbon disulfide were added to the reaction flask, heated to reflux, reacted for 2 hours, cooled to 25°C, filtered, and the filtrate was adjusted with 1 wt% hydrochloric acid to precipitate Substance 18. Filter, wash, and dry to obtain substance eighteen;

[0043] Synthesis of Substance 20: Add Substance 18, Substance 19, Toluene and Potassium Carbonate to the reaction flask, reflux, cool and filter, wash the solid with dichloromethane, concentrate the filtrate under reduced pressure, and the residue is chromatographed on silica gel. Elution with alkane-ethyl acetate gave substance 20.

[0044] Synthesis of compound III: add substance 20, 4-fluorobenzyl chloride, NaOH, acetonitrile to the reaction flask, reflux reaction, cool, and evaporate the solvent under reduced pressure to obtai...

Embodiment 3

[0050]The method for the compound described in synthetic embodiment 1, described synthetic route is described in embodiment 2:

[0051] Synthesis of Substance 18: Substance 17, KOH, water, and carbon disulfide were added to the reaction flask, heated to reflux, reacted for 8 hours, cooled to 25°C, filtered, and the filtrate was adjusted with 10 wt% hydrochloric acid to precipitate Substance 18, Filter, wash, and dry to obtain substance eighteen;

[0052] Synthesis of Substance 20: Add Substance 18, Substance 19, Toluene and Potassium Carbonate to the reaction flask, reflux, cool and filter, wash the solid with dichloromethane, concentrate the filtrate under reduced pressure, and the residue is chromatographed on silica gel. Elution with alkane-ethyl acetate gave substance 20.

[0053] Synthesis of compound III: add substance 20, 4-fluorobenzyl chloride, NaOH, acetonitrile to the reaction flask, reflux reaction, cool, and evaporate the solvent under reduced pressure to obtain ...

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PUM

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Abstract

The invention belongs to the field of biomedicines, and especially relates to an application of a compound in the preparation of kallikrein KLK7 inhibition medicines, and a synthesis method of the compound. The structural formula of the compound is shown in the description. The compound for inhibiting the kallikrein KLK7 can effectively inhibit the activity of the KLK7, the synthesis method of the compound is simple and is easy to implement, and proper auxiliary materials and assistants can be added to prepare medicinal preparations for inhibiting the activity of the KLK7.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to the application and synthesis method of compounds in the preparation of drugs for inhibiting kallikrein KLK7. Background technique [0002] Atopic dermatitis (Atopic Dermatitis, AD) is a widespread chronic inflammatory skin disease, characterized by dry, scaly skin, inflammation, and increased skin permeability. Harmless elements can also be sensitive to surface infection. The incidence of atopic dermatitis in industrialized countries has increased two to threefold over the past 30 years, with an estimated prevalence of 15–30% in children and 10% in adults. up 2-10%. Due to the complexity of the pathogenesis, the pathogenesis of AD is not well understood, but skin barrier dysfunction has been confirmed to be one of the key factors in the development of AD. The stability of the skin barrier depends on the balance between the differentiation of keratinocytes in the granula...

Claims

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Application Information

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IPC IPC(8): A61K31/444A61P17/00A61P29/00C07D471/04
CPCA61K31/4245A61K31/427A61K31/444A61K31/519A61K31/5377C07D471/04A61K2300/00
Inventor 谭潇刘森杨丽婷
Owner CHINA THREE GORGES UNIV