单胺菌素─喹诺酮酰胺衍生物的合成

SynthesisofMonobactam┐QuinoloneAmideDerivatives

为探索喹诺酮类化合物充当单胺菌素３位边链酸的构效关系，合成了４个未见文献报道的单胺菌素－喹诺酮酰胺衍生物（５ａ）～（５ｄ）．它们是以氧氟沙星（８）、氟罗沙星（９）或诺氟沙星前体（１－乙基－６－氟－７－氯－１，４－二氢－４－氧代喹啉－３－羧酸）（１０）通过ＤＣＣ－ＨＯＢＴ法酰化卡芦莫南母核（６）或氨曲南母核（７）得到的．

Thesynthesisoffournovelmonobactams(5a)～(5d)inaneforttoexploretheroleofquinoloneasmonobactamC-3side-chainacidwasdescribed.Theywereaffordedbyacylat-ingcarumonamnucleus(6)oraztreonamuncleus(7)withofloxacin(8),fleroxacin(9)ornorfloxacinprecursor,7-chloro-1-ethyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylicacid(10),accordingtostandardDCC-HOBTmethodology.Inpreliminaryinvitroantibacterialbioassay,noneofthefourtitlemonobactamswereactiveuptoconcentrationof100mg/L.