One class of light affinity labelling double function probe molecules, preparing and use

A probe molecule and bifunctional technology, applied in a class of photoaffinity labeled bifunctional probe molecules, preparation and application fields, can solve a wide range of problems such as incomplete activity

Inactive Publication Date: 2007-01-24
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It has been reported in the literature that the target of some of its pharmacological effects is adenosine receptors. From the existing pharmacological research, it is obviously incomplete to try to explain its wide range of activities with a single drug target

Method used

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  • One class of light affinity labelling double function probe molecules, preparing and use
  • One class of light affinity labelling double function probe molecules, preparing and use
  • One class of light affinity labelling double function probe molecules, preparing and use

Examples

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Embodiment Construction

[0047] The following examples illustrate the probe molecules covered by the present invention and their design, preparation, and application, but here are only examples and do not limit the present invention.

[0048] Preparation of compound 1:

[0049]

[0050] Paeoniflorin (0.720g, 1.5mmol) and imidazole (1.224g, 18.00mmol) were dissolved in 30mL DMF, and TBSCl (1.356g, 9.00mmol) was added at 0°C. After stirring at room temperature for 12 hours, the reaction was completed, and 30 mL of H 2 O, extracted with 3×50mL ether, combined the organic layers, washed with 3×30mL saturated brine, separated the organic layer, anhydrous Na 2 SO 4 dry. Silica gel column chromatography (petroleum ether: ethyl acetate = 3:1) gave 0.670 g of a colorless oily substance, with a yield of 63.0%.

[0051] 1 H NMR (300MHz, CD3OD): δ0.92(18H), 0.11(12H), 1.36(3H), 1.82(1H), 1.90(1H), 2.09(1H), 2.52(1H), 2.59(1H), 3.12-3.38(3H), 3.68(1H), 3.95(1H), 4.48(1H), 4.75(2H), 5.42(1H), 7.48(2H), 7.6...

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Abstract

The present invention discloses preparation process and application of light affinity labeling double function probe molecule in the structural expression as shown. The probe molecule is used in screening penoniflorin and similar compounds for correlative proteinogram research and in researching and finding the action target sport, action mode, active site and other structure information of active compound penoniflorin. The present invention provides important way for searching penoniflorin and similar compounds.

Description

field of invention [0001] The invention relates to the design and synthesis of a class of photoaffinity-labeled bifunctional probe molecules for paeoniflorin, an active component of traditional Chinese medicine with neuroprotective effect, and its application in searching for new drugs. Paeoniflorin is an active ingredient isolated from the traditional Chinese herb Paeoniae officinalis, which has many pharmacological effects. The probe molecules involved in the present invention can be used to screen active compounds of paeoniflorin; to conduct research on related protein profiles; Structural information, providing important information for the discovery of such drugs. The invention also relates to the structural design and preparation method of the probe molecule. Background of the invention [0002] The process of finding new drugs includes many stages such as: target identification, lead compound discovery, structure optimization of small molecule compounds, preclinical...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/04G01N33/52G01N33/68G01N33/15
Inventor 南发俊李佳叶阳朱兴族李静雅仇文卫徐杰
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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