《高等药物化学》课程教学资源（PPT课件讲稿）Chemotherapeutic Agents

Anti-infectives A∥ rights re served Chemotherapeutic Agents Anticancer Antiparasite Anti-infectives MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Chemotherapeutic Agents ▪ Anticancer ▪ Antiparasite ▪ Anti-infectives

Anti-infectives A∥ rights re served Totally Synthesized Antibacterials sulfonamides and the synerists fluoroquinolones oxazolidinones嵁唑烷酮类 MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Totally Synthesized Antibacterials ▪ sulfonamides and the synerists ▪ fluoroquinolones ▪ oxazolidinones噁唑烷酮类

Anti-infectives A∥ rights re served Fluoroquinolone antibacterials Discovery history Marketed products Action mechanism Structure-activity and structure toxicity relationships New progress Synthesis MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Fluoroquinolone antibacterials ▪ Discovery history ▪ Marketed products ▪ Action mechanism ▪ Structure-activity and structure￾toxicity relationships ▪ New progress ▪ Synthesis

Anti-infectives A∥ rights re served Discovery history CH3 NHCH(CH2)3N(C2H5)2 CO,H Structural modification H3C C2h4 chloroquine nalidixic acid malarial O CO,H CO,H HN N C2H norfloxacin pipemidIc acid generation 2 generation 3 MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Discovery history N NHCH(CH2 )3N(C2H5 )2 CH3 Cl Structural modification N N C2H5 CO2H O H3C chloroquine antimalarial nalidixic acid N N N O CO2H C2H5 HN N N O CO2H C2H5 HN N F generation 1 pipemidic acid generation 2 norfloxacin generation 3

Anti-infectives A∥ rights re served Marketed products 19个:诺氟沙星,培氟沙星,环丙沙星, 氧氟沙星,依诺沙星,洛美沙星,托氟沙 星,氟罗沙星,卢氟沙星,那氟沙星,左 氟沙星,司氟沙星,曲伐沙星,加替沙星 莫西沙星,帕珠沙星,吉米沙星,巴洛 沙星,普利沙星 兽药6个:达诺沙星,二氟沙星,恩氟沙 星,麻保沙星,奥比沙星和沙拉沙星 MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Marketed products ▪ 19个：诺氟沙星，培氟沙星，环丙沙星， 氧氟沙星，依诺沙星，洛美沙星，托氟沙 星，氟罗沙星，卢氟沙星，那氟沙星，左 氟沙星，司氟沙星，曲伐沙星，加替沙星 ，莫西沙星，帕珠沙星，吉米沙星，巴洛 沙星，普利沙星 ▪ 兽药6个：达诺沙星，二氟沙星，恩氟沙 星，麻保沙星，奥比沙星 和沙拉沙星

Anti-infectives A∥ rights re served Marketed products 1 R R norfloxacin F CooH pefloxacin Et Me R一N N ciproflo H R MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Marketed products 1 N O COOH R1 N N F R norfloxacin Et H pefloxacin Et Me ciprofloxacin H R1 R

Anti-infectives A∥ rights re served Marketed products 2 R F、 R COOH R一N F RI R R Rs R R R lomefloxacin Et HH CH fleroxacin CH CHF H CH3 H H sparfloxacin NH2 H CH3 CH3 MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Marketed products 2 N O COOH R1 N N F R F R5 R' R'' R1 R5 R R' R'' lomefloxacin Et H H CH3 H fleroxacin CH2CH2 F H CH3 H H sparfloxacin NH2 H CH3 CH3

Anti-infectives A∥ rights re served Marketed products 3 R 7 CH gatifloxacin NH F moxifloxacin H COOH N H R OMe balofoxacin NHCH MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Marketed products 3 N O COOH F OMe R7 gatifloxacin N NH CH3 moxifloxacin H N H H H balofloxacin N NHCH3 R7

Anti-infectives A∥ rights re served Marketed products 4 R R ofloxacin CH3(R,S) NCH CooH levofloxacin CH3 (S) NCH R rufloxacin H NCH3 R nadifloxacin CH3(,S) 〉OH NH pazufloXacin CH3(S) MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Marketed products 4 N O COOH F R7 X R N NCH3 R7 ofloxacin CH3 (R,S) O R X levofloxacin CH3 (S) N NCH3 O N NCH3 rufloxacin H S N OH CH2 nadifloxacin CH3 (R,S) pazufloxacin CH3 (S) NH2 O

Anti-infectives A∥ rights re served Marketed products 5 R R tosufloxacin F COOH CH,NH, R gemifloxacin NOCH H rovanoxacin NH H enoXacin Et NH MP士海医药工业研究院 NDUSTRY

Anti-infectives All rights re served Marketed products 5 N N O COOH F R7 R1 tosufloxacin F F N NH2 gemifloxacin N CH2NH2 NOCH3 R1 R7 F F N NH2 H H trovafloxacin enoxacin Et N NH