Preparation and application of berberine derivative with IDO1/TDO inhibitory activity

The invention discloses a berberine derivative and a preparation method thereof, and application of the berberine derivative as an IDO1/TDO inhibitor. A series of heteroatom-containing high-B-ring berberine derivatives are efficiently prepared by combining a C-H activation/cyclization method, the he...

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Bibliographic Details
Main Authors JIA PENGFEI, LYU SHAN, WU YONG, CHEN KANG, HAI LI, LU JIAQI, LI GUOBO, NING XIANGLI, LAI RUIZHI
Format Patent
LanguageChinese
English
Published 12.07.2022
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The invention discloses a berberine derivative and a preparation method thereof, and application of the berberine derivative as an IDO1/TDO inhibitor. A series of heteroatom-containing high-B-ring berberine derivatives are efficiently prepared by combining a C-H activation/cyclization method, the heteroatom-containing high-B-ring berberine derivatives comprise novel isoquinoline quaternary ammonium base derivatives with A or D rings being thiophene rings, in addition, berberine derivatives are prepared by utilizing a novel method of introducing ethoxyl into epoxypropane, and the heteroatom-containing high-B-ring berberine derivatives can be used for preparing high-B-ring berberine derivatives. The prepared berberine derivative has very high inhibitory activity on IDO1/TDO enzyme. The compound can be used for treating or preventing cancers or tumors, metabolic disorder diseases, autoimmune diseases, Alzheimer's disease, Parkinson's disease, depression and other related diseases. 本发明公开一种小檗碱衍生物及其制备方法，和其作为IDO1/TD
Bibliography:Application Number: CN202210415635