Quinolones 喹诺酮类 andUrinary Tract Antiseptics
Quinolones 喹诺酮类 and Urinary Tract Antiseptics
OverviewA new synthetic antibacterial drug was patented in 1962:nalidixicacid,ineffective against systemic infections,but useful againsturinary infectionsItsoverusehasnowledOHtomanyresistances,butithasbeenthebasisformoredrugdevelopmentHnalidixic acid2
2 Overview A new synthetic antibacterial drug was patented in 1962: nalidixic acid, ineffective against systemic infections, but useful against urinary infections Its overuse has now led to many resistances, but it has been the basis for more drug development
氟喹诺酮类1. FluoroguinolonesantibacterialOHactivitymembrane-fixationsitespenetrationnalidixicH3C&gyraseacidRSinhibitionFOHROHglobalRspectrumantibacterialactivityanaerobesRpyrridone β carboxylic acidFluorination enhanced cell penetration and activity3
3 1. Fluoroquinolones 氟喹诺酮类 Fluorination enhanced cell penetration and activity
Mechanism of ActionchromosomesupercoiledRNA coreRNAcoreDNAgyrasechromosomefoldedearoundRNAcore个quinolonesQuinolonesinhibitthereplicationofbacterial DNAbyinterfering withthe indispensableactionoftheDNAgyrase(topoisomeraseIl)
4 Mechanism of Action Quinolones inhibit the replication of bacterial DNA by interfering with the indispensable action of the DNA gyrase (topoisomerase II)
Entry into BacteriumFluoroguinolones are water-soluble drugs. They enter thebacteriumthroughporins,orwater-filled channelsintheoutermembraneofGram-negativebacteriaThis acounts fortheir higherefficiencyagainst Gram-negativemicro-organisms5
5 Entry into Bacterium Fluoroquinolones are water-soluble drugs. They enter the bacterium through porins, or water-filled channels in the outer membrane of Gram-negative bacteria This acounts for their higher efficiency against Gramnegative microorganisms