Biological orthogonal broken bond reaction system, prodrug and application

The invention discloses a biological orthogonal broken bond reaction system, a prodrug and application. In existing biological orthogonal reaction types, tetrazine and trans-ene are optimal systems applied to drug delivery at present, but have the defect of instability; the invention discloses a nov...

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Bibliographic Details
Main Authors JI XINGYUE, YAN ZHICHENG, KOEHENT, JIAO GUOFENG
Format Patent
LanguageChinese
English
Published 01.09.2023
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
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 biological orthogonal broken bond reaction system, a prodrug and application. In existing biological orthogonal reaction types, tetrazine and trans-ene are optimal systems applied to drug delivery at present, but have the defect of instability; the invention discloses a novel biological orthogonal bond breaking reaction, N-oxide can quickly react with an organic silicon boric acid derivative under a quasi-physiological condition to obtain corresponding tertiary amine and silanol, the reaction has the characteristics of quick reaction kinetics, simple and easily available reaction components and the like, and the secondary reaction kinetics constant k2 can reach 103 M <-1 > s <-1 >. A corresponding intelligent fluorescent probe or prodrug containing a tertiary amine functional group is designed by utilizing a biological orthogonal bond breaking reaction, is very stable under physiological conditions, and generates corresponding tertiary amine after being subjected to a click reaction
Bibliography:Application Number: CN202310434063