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Phosphodiesterase PDE2 activity inhibitor

An activity inhibitor, the technology of phosphodiesterase, which is applied in the field of medicine and achieves the effect of good PDE2 enzyme inhibition effect

Inactive Publication Date: 2020-11-27
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing PDE2 inhibitors mainly include EHNA, BAY60-7750, and dipyridamole, etc., but no drugs have been marketed yet

Method used

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  • Phosphodiesterase PDE2 activity inhibitor
  • Phosphodiesterase PDE2 activity inhibitor
  • Phosphodiesterase PDE2 activity inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] 1-Ethyl-2-oxo-1,2-dihydro-benzo[cd]indole-6-sulfonic acid (4-fluoro-phenyl)-amide (SPECS library number: AQ-390 / 40910475) through AMP kit detects its enzymatic level IC 50 The value is 6.098±2.619μmol / L (such as figure 1 shown), and by PDE-Glo TM Phosphodiesterase Assay to detect its enzymatic level IC 50 The value is 3.554±0.396μmol / L (such as figure 2 shown), has a good PDE2 enzyme inhibitory effect

Embodiment 2

[0063] 1-Ethyl-N-(furan-2-ylmethyl)-2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide via Alph AMP kit detects its enzymatic level IC 50 The value is 24.49±3.03μmol / L (such as image 3 shown), and by PDE-Glo TM Phosphodiesterase Assay to detect its enzymatic level IC 50 The value is 17.56±3.68μmol / L (such as Figure 4 Shown), has a good PDE2 enzyme inhibitory effect.

Embodiment 3

[0065] N-(3,4-dimethoxybenzyl)-1-ethyl-2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide via A AMP kit detects its enzymatic level IC 50 The value is 22.16±1.36μmol / L (such as Figure 5 shown), and by PDE-Glo TM Phosphodiesterase Assay to detect its enzymatic level IC 50 The value is 17.76±1.1μmol / L (such as Figure 6 Shown), has a good PDE2 enzyme inhibitory effect.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a phosphodiesterase PDE2 activity inhibitor. A sulfonamide compound or at least one of hydrate, pharmaceuticallyacceptable salt, tautomer, stereoisomer and precursor compound of the sulfonamide compound is used as an active ingredient for preparing a medicine for preventing or treating the PDE2 disorder. The sulfonamide compound selected by the invention can effectively inhibit the activity of the PDE2 enzyme, and detection of the enzyme level IC50 value of the sulfonamide compound by kit and PDE-GloTMPhosodiesterase Assay shows that the sulfonamide compound has a good PDE2 enzyme inhibition effect. The compound disclosed by the invention is used as an effective inhibitor of PDE2, is expected to be usedas an active ingredient for preparing a medicine for treating PDE2 disorder, and has a medicinal prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an inhibitor of phosphodiesterase PDE2 activity. Background technique [0002] In 1958, Rall and Sutherland et al. first discovered cyclic adenosine monophosphate (Cyclic adenosine 3', 5'-monophosphate, cAMP); in 1963, Ashman et al. discovered cyclic guanosine monophosphate (cGMP) . Since then, the research on cyclic adenosine monophosphate and cyclic guanosine monophosphate has received more and more attention. [0003] Cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) regulate gene expression by controlling ion channels in cells, are important second messengers in cells, and are related to the realization of many physiological functions, such as learning and memory , cell cycle regulation, cell differentiation, proliferation, inflammatory processes, smooth muscle contraction and relaxation, visual signal transduction and metabolic fu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/92C07D405/12A61K31/635A61P25/00A61P25/30A61P25/04A61P25/18A61P25/22A61P25/14
CPCA61P25/00A61P25/04A61P25/14A61P25/18A61P25/22A61P25/30C07D209/92C07D405/12
Inventor 宋国强高英孔韧唐龙黄险峰冯筱晴谈颖夏颜
Owner CHANGZHOU UNIV