代表药物R20药物名称RR2R3R49Z8123奥沙西洋OxazepamCIHHOHR3ABR1替马西泮CIHOHCH561'TemazepamR4劳拉西洋LorazepamCIHCI2OHC硝西泮HHHNO2Nitrazepam氯硝西洋HHCINO2ClonazepamF氟西洋FlurazepamCICH3HCH3F氟地西洋CIHCH3Fludiazepam
代表药物 N N R1 O R3 R2 R4 1 2 3 5 4 6 1' 2' 7 8 9 A B C N CH3 CH3 药物名称 R1 R2 R3 R4 奥沙西泮Oxazepam Cl H OH H 替马西泮 Temazepam Cl CH3 OH H 劳拉西泮Lorazepam Cl H OH Cl 硝西泮 Nitrazepam NO2 H H H 氯硝西泮 Clonazepam NO2 H H Cl 氟西泮Flurazepam Cl H F 氟地西泮 Fludiazepam Cl CH3 H F
构效关系1位和2位拼入三氮唑可提高稳定性R1R2艾司唑仑HHH阿普唑仑CH3NCCI三唑仑CH3R2活性均比地西洋强几十倍
构 效 关 系 1位和2位拼入三氮唑可提高稳定性 Cl N R2 N N N R1 H H H Cl 艾司唑仑 阿普唑仑 三唑仑 R1 R2 CH3 CH3 活性均比地西泮强几十倍
构效关系4.5-位拼入含氧的嗯唑环增加药物的稳定性R2R1R4R3嗯唑仑CH3CIHHNFHH卤嗯唑仑BrR3H美沙唑仑CICH3CIR4R2
构 效 关 系 4,5-位拼入含氧的噁唑环增加药物的稳定性 N R1 H O N O R3 R2 Cl H H Br F H Cl CH3 噁唑仑 卤噁唑仑 美沙唑仑 R1 R2 R3 Cl R4 R4 CH3 H H
构效关系生物电子等排体仍有较好的镇静催眠作用CF3C0溴替唑仑R=BrRFNCIF依替唑仑ENR=C2H5CI夸西洋
构 效 关 系 生物电子等排体仍有较好的镇静催眠作用 N S N Cl R R=Br R=C2 H5 N N S F 夸西泮 溴替唑仑 依替唑仑 Cl CF3 N H3 C N
代谢Metabolismprogress mainly inLiversimilar with Barbiturates中N-demethylation;Ring scission at 1,2 position;Hydroxylationat C-3;phenolic hydroxylation at phenolic hydroxylReduction of nitrogen oxides;
代 谢 Metabolism progress mainly in Liver similar with Barbiturates N-demethylation； Ring scission at 1，2 position; Hydroxylation at C-3； phenolic hydroxylation at phenolic hydroxyl； Reduction of nitrogen oxides;