典型文献
Discussion on the dimerization reaction of penicillin antibiotics
文献摘要：
Penicillins are one type of the most important antibiotics used in the clinic.Control of drug impurity profiles is an important part of ensuring drug safety.This is particularly important in penicillins where polymerization can lead to polymers as elicitors of passive cutaneous anaphylaxis.The current under-standing of penicillin polymerization is based on reactions with amino groups,but no comprehensive mechanistic understanding has been reported.Here,we used theoretical calculations and column switching-LC/MS techniques to study penicillin dimerization.Ampicillin and benzylpenicillin were selected as representative penicillins with or without amino groups in the side chain,respectively.We identified four pathways by which this may occur and the energy barrier graphs of each reaction process were given.For benzylpenicillin without an amino group in the 6-side chain,dimerization mode A is the dominant mode,where the 2-carboxyl group of one molecule reacts with the β-lactam of another molecule.However,ampicillin with an amino group in the 6-side chain favors dimerization mode C,where the amino group of one molecule attacks the β-lactam of another molecule.These findings can lead to a polymer control approach to maintaining penicillin antibiotics in an active formulation.
文献关键词：
中图分类号：
作者姓名：
Qizhang Wu;Xia Zhang;Jiaxin Du;Changqin Hu
作者机构：
National Institutes for Food and Drug Control,Beijing,102629,China
文献出处：
引用格式：
[1]Qizhang Wu;Xia Zhang;Jiaxin Du;Changqin Hu-.Discussion on the dimerization reaction of penicillin antibiotics)[J].药物分析学报（英文）,2022(03):481-488
A类：
Penicillins,penicillins,elicitors,Ampicillin,benzylpenicillin
B类：
Discussion,dimerization,antibiotics,are,one,type,most,important,used,clinic,Control,drug,impurity,profiles,ensuring,safety,This,particularly,where,polymerization,can,lead,polymers,passive,cutaneous,anaphylaxis,current,reactions,amino,groups,but,comprehensive,mechanistic,understanding,has,been,reported,Here,theoretical,calculations,column,switching,LC,techniques,study,were,selected,representative,without,side,chain,respectively,We,identified,four,pathways,by,which,this,may,occur,energy,barrier,graphs,each,process,given,For,mode,dominant,carboxyl,molecule,reacts,lactam,another,However,ampicillin,favors,attacks,These,findings,control,approach,maintaining,active,formulation
AB值：
0.476959
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