Pentacyclic triterpenoid TGR5 receptor stimulant, preparation method and application thereof

A heterocyclic and cycloalkyl technology, applied in the field of TGR5 agonists, can solve the problems of difficult preparation, insufficient permeability, harsh multi-step reaction conditions, etc., and achieve the effect of abundant natural sources, simple synthesis method, and excellent agonistic activity
CN112694514AActive Publication Date: 2021-04-23SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Publication Date
2021-04-23

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Abstract

The invention discloses a pentacyclic triterpenoid TGR5 receptor stimulant, a preparation method and application of the pentacyclic triterpenoid TGR5 receptor stimulant. The structure of the pentacyclic triterpenoid TGR5 receptor stimulant is as shown in a formula I, and the definition of each substituent is as shown in the specification and claims. According to the pentacyclic triterpenoid compound, the solubility is increased, the permeability is improved, the TGR5 receptor agonist activity is remarkably improved, Caco-2 monolayer cells can be penetrated, and the in-vivo drug effect exertion of the compound after oral administration is guaranteed. The TGR5 receptor stimulant is expected to be further developed into a medicine for treating metabolic diseases represented by diabetes.
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Description

technical field

[0001] The present invention relates to a class of TGR5 (bile acid G protein-coupled receptor) agonists, specifically, to a class of pentacyclic triterpenoids, a preparation method thereof, and the TGR5 receptor agonist or its pharmaceutical Use of acceptable salts or pharmaceutical compositions containing any one of them in the preparation of medicines for treating diabetes, obesity, hyperlipidemia, liver damage and inflammatory diseases. Background technique

[0002] TGR5 is a G protein-coupled receptor that can be activated by bile acids and is named membrane bile acid receptor (M-BAR) or TGR5. TGR5 is highly expressed in gallbladder, bile duct epithelial cells, brown adipose tissue, muscle, intestine, kidney, placenta and brain. When the ligand binds to TGR5, it will activate adenylate cyclase, which will increase the level of intracellular cAMP and show different physiological effects in different tissues. In the small intestine, the increase of cAMP l...

Claims

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