Synthesis And In Situ Pharmacodynamic Activiti Analysis Of Nitrogen Heterocyclic Compounds Based On ICT

Complex life activities have always been an important research area in the scientific community.Studying human life activities can not only understand the causes of diseases,but also treat specific diseases.At present,there are various treatment methods for diseases,such as drug therapy,light therapy,physical therapy,etc.However,among the many treatment methods,the most widely used is still drug treatment.Most drugs need to enter the body to function.However,due to the limitations of the human body,we cannot observe and analyze the drug’s pharmacodynamic activity and action pathways well.Therefore,we need to analyze the drug’s pharmacodynamic activity through appropriate methods.Most of the common analytical methods act on the drug itself for analysis in vitro,and the fluorescent imaging analysis method is widely used in drug analysis at the biological cell level because of its excellent sensitivity,efficient space-time resolution,and bioimaging penetration ability.Organic fluorescent small molecules combined with microscopic imaging for the fluorescent imaging analysis has become a popular method for drug analysis in recent years.Based on the excellent application prospect of fluorescent imaging analysis method,this paper has been carried out to construct and construct a drug efficacy evaluation in the human body.This paper carried out two studies,the first is construction of nitrogen heterocyclic compounds for detecting p Hi based on ICT principle,and second section is construction of nitrogen heterocyclic compounds based on ICT,make it combined with erlotinib via click reaction and analyze the pharmacodynamic activity of erlotinib in cells.There are many factors that affect life activities in the intracellular environment.Among them,intracellular p H(p Hi)is a very important physical and chemical factor,which affects the basic life activities of the body and also plays a vital role in the exploration and treatment of diseases.When the cells enter an irreversible process of programmed death,p Hi will become stable without reversible changes.Therefore,in order to be able to monitor this physicochemical property,in our first work,based on the mechanism of intramolecular charge transfer,a class of nitrogen heterocyclic compounds with specific groups were constructed,which can be used to monitor the intracellular p Hi in real time.Molecule(UV-SP).In our work,we proved that UV-SP has sensitive response to changes in intracellular p Hi,and not easily interfered by other factors in the intracellular environment,has good stability and selectivity,and can specifically recognize p Hi and monitoring.This indicates that the compound UV-SP can detect whether the cell enters programmed death by monitoring the change of p Hi.In order to evaluate whether the anti-tumor drug exerts a drug effect in the body to kill cancer cells,the process of inducing cancer cell to enter programmed death took a new direction.Erlotinib is a drug for the treatment of non-small cell lung cancer,in order to study its action process in the human body and evaluate its pharmacodynamic activity,in the second work,we designed and synthesized the nitrogen heterocyclic compounds based on ICT as a fluorescent compound(UW)for the analysis of the drug efficacy.UW uses acenaphthene quinone as the parent,and after modification,it has an azide group can react with the terminal alkynyl group of Erlotinib in Click reaction.After testing and analyzing UW,we found that UW can undergo cycloaddition reaction with erlotinib,and the structure of the resulting compound E is stable and not easy to be destroyed.After related tests in vitro,UW shows its good stability and biocompatibility,and has a strong fluorescent signal.After the testing in vitro,we conducted related biological tests on UW.In cell imaging tests,UW showed better fluorescence signal intensity and imaging ability than erlotinib.The results of the vitro testing and cell imaging laid the foundation for related biological tests after UW and drugs were combined in vivo.