Indolebenzamide derivatives and medicinal applications thereof

By constructing dopamine and 5-HT1A receptor models, we screened out highly active small molecule compounds of indolinamide derivatives, which solved the problems of poor efficacy and side effects of existing antischizophrenia drugs on negative symptoms, and achieved the goal of treating 5-HT1A receptors. -Effective inhibition of HT1A receptors provides new drugs for the treatment of neuropsychiatric diseases.

CN102372659AInactive Publication Date: 2012-03-14FUDAN UNIVERSITY +1
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Patent Information

Application Number
CN201010254261.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2010-08-16
Publication Date
2012-03-14
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing antischizophrenia drugs have poor efficacy on negative symptoms and have side effects, such as extrapyramidal symptoms and granulocytopenia. It is of great significance to develop new 5-HT1A receptor antagonists with low toxicity and side effects.

Method used

Using the crystal structure of adrenergic β2 receptor as a template to construct dopamine receptor and 5-HT1A receptor models, through molecular dynamics simulation and active site detection, small molecule compounds of indole benzamide derivatives with high activity were screened out. For the preparation of 5-HT receptor inhibitors.

Benefits of technology

The obtained compound has an inhibitory effect on 5-HT1A receptors and has the potential to be used to treat neuropsychiatric diseases such as schizophrenia and Parkinson's disease caused by dysfunction of the dopamine and 5-HT systems, providing a novel structure, low toxicity and side effects. Treatment options.

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Abstract

The invention belongs to the biopharmaceutical field and relates to indolebenzamide derivatives and applications thereof in the preparation of the 5-HT receptor inhibitor, in particular to the affinities and action characteristics of the indolebenzamide derivatives to the 5-HT1A receptor and applications thereof in the preparation of nervous system disease medicines, particularly applications thereof in the nervous system disease medicine field related to the 5-HT receptor. The result of biological tests shows that the indolebenzamide derivatives can inhibit the 5-HT1A receptor which is related to the pathology of nervous and mental system diseases. The compounds can be used as medicinal lead compounds to synthesize the 5-HT receptor inhibitor and further used to prepare the medicines for nervous and mental system diseases such as schizophrenia and parkinsonism which are caused by the disfunctions of the dopamine system and the 5-HT system.
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