((人工合成人工合成(rénōnhéchén)ɡɡɡ(rénōnhéchén)ɡɡɡ抗菌药抗菌药))HuifangTang第一页，共五十四页。Syntheticantimicrobialagents•Ⅰ.Quinolones(喹诺酮类);•Ⅱ.Sulfonamides(磺胺类);•Ⅲ.Othersyntheticantimicrobialagents:•Trimethoprim(甲氧苄啶)•Nitrofurans(硝基(xiāojī)呋喃类),etc.第二页，共五十四页。Generalfeatures•Broadantimicrobialactivityandareeffectiveafteroraladministrationforthetreatmentofawidevarietyofinfectiousdisease.•Relativelyfewsideeffects.•Microbialresistancetotheiractiondoesnotdeveloprapidly.QuinolonesQuinolones第三页，共五十四页。Chemistry•Derivedfrombasicstructureofnalidixicacid(萘啶酸)andhavesubstituentsatN-1,C-5,C-7,position8andafluorineatomatposition6.•Fluorineatposition6enhancesgyraseinhibitionandcellpenetration.QuinolonesQuinolonesQuinolones第四页，共五十四页。ChemicalstructureQuinolones((诺氟沙星诺氟沙星))((环丙沙星环丙沙星))((萘啶酸萘啶酸))Quinolones第五页，共五十四页。GenerationExamples1st(1962-1969)Nalidixicacid,萘啶酸2nd(1969-1979)Pipemidicacid吡哌酸Cinoxacin西诺沙星3rd(1980-1996)Norfloxacin诺氟沙星Levofloxacin左氧氟沙星Ciprofloxacin环丙沙星Ofloxacin氧氟沙星sparfloxacin司帕沙星4th(1997-)Grepafloxacin格帕沙星Clinafloxacin克林沙星Gatifloxacin加替沙星Moxifloxacin莫西沙星Quinolones第六页，共五十四页。第七页，共五十四页。第八页，共五十四页。First-generationagents(1962-1969)First-generationagents(1962-1969)Nalidixicacid,Nalidixicacid,萘啶酸萘啶酸•ThefirstgenerationdrugofthequinoloneantibioticsThefirstgenerationdrugofthequinoloneantibiotics•Moderategram-negativeactivityandminimalsystemicdistributionModerategram-negativeactivityandminimalsystemicdistributionClinicalapplicationsClinicalapplications•UncomplicatedurinarytractinfectionsUncomplicatedurinarytractinfectionsQuinolonesQuinolonesQuinolones第九页，共五十四页。Second-generationquinolonesSecond-generationquinolones(1969-1979)(1969-1979)PipemidicacidPipemidicacid吡哌酸吡哌酸CinoxacinCinoxacin西诺沙星西诺沙星•Expandedgram-negativeactivityandatypicalpathogencoverage,butlimit...
