A steroidal derivative containing a pyrazole-thiazolinone heterocycle and its preparation method and application
By designing steroid derivatives containing pyrazole-thiazolinone heterocycle, the problems of insufficient activity and great toxicity of existing glucocorticoid compounds are solved, and effective inhibition of inflammatory response and low toxicity are achieved.
CN119775337APending Publication Date: 2025-04-08CANCER HOSPITAL AFFILIATED TO SHANTOU UNIV SCHOOL OF MEDICINE
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Patent Information
- Application Number
- CN202311290669.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2023-10-07
- Publication Date
- 2025-04-08
AI Technical Summary
Technical Problem
The activity of existing glucocorticoid compounds is not high enough and have high toxicity, which limits their application in clinical practice.
Method used
A class of steroid derivatives containing pyrazole-thiazolinone heterocycles with novel structures were designed. By introducing dihydropyrazole and thiazolinone units, the biological activity and selectivity of the compounds were improved and the toxicity was reduced.
Benefits of technology
This compound had a significant inhibitory effect on the inflammatory response of LPS-induced BV2 microglia and RAW264.7 mice peritoneal macrophages, showing excellent anti-inflammatory activity and low cytotoxicity.
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Abstract
The present invention discloses a steroidal derivative containing a pyrazole-thiazolinone heterocycle and its preparation method and application. The steroidal derivative containing a pyrazole-thiazolinone heterocycle of the present invention has a strong inhibitory effect on nitric oxide (NO) produced by lipopolysaccharide (LPS)-induced RAW 264.7 mouse peritoneal macrophages and BV2 mouse microglial neurons, especially the anti-inflammatory activity of compound 5 prepared by the preparation method is better than dexamethasone, and the toxicity is less than dexamethasone, and the effect of different substituents on the inhibitory activity can be combined to expand the in-depth application of steroidal derivatives of pyrazole-thiazolinone heterocycles in fighting inflammation. The compound of the present invention is simple to prepare, and the raw materials are easy to obtain. More importantly, it has good anti-inflammatory activity and lower cytotoxicity, which is of great significance in the preparation of drugs for preventing and treating inflammation / neuroinflammation or autoimmune-related diseases.
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