1、A Free sample background from Slide 1第九章 化学治疗药Chemotherapeutic Agents A Free sample background from Slide 2第二节 抗结核药物(Tuberculostatics)抗结核药物分类合成抗结核药抗结核抗生素A Free sample background from Slide 3一、合成抗结核药物 异烟肼(Isoniazid) NO N NH2H4-吡啶甲酰肼( 4-Pyridinecarboxylic acid hydrazide) A Free sample background from
2、Slide 4异烟肼的发现N N NH2H3COHN SHNCONHNHCSNH2NO N NH2H氨硫脲(Thioacetazone) 异烟醛缩氨硫脲(Isonicotinaldehyde thiosemicarbazone) A Free sample background from Slide 5异烟肼衍生物异烟肼的N2取代的衍生物具有抗结核活性，而N1取代衍生物则无抗结核活性。所有的Isoniazid衍生物其抗结核活性低于Isoniazid。NCONHNH=CH OHOCH3异烟腙(Ftivazide ) NN N OHOOOHOHOH葡烟腙 (Glyconiazide) A Free
3、 sample background from Slide 6NN N OCaO N NOO OONCH3 CH3H H丙酮酸异烟腙钙(Pyruvic Acid calcium Ftivazide) A Free sample background from Slide 7异烟肼作用机理 NNOHNH2KateGMn2+具有酰化活性的中间体NHONHH2NONADHA Free sample background from Slide 8异烟肼作用机理 酰化剂NO N NH2HKatGNO HNO OHNO NH2NO N NHNONO O OO2NO O OH过氧化氢酶-过氧化物酶异烟酰自由
4、基 过氧烟酸异烟醛 异烟酰胺异烟酸A Free sample background from Slide 9异烟肼的代谢NO N NH2HNO N N=CHCOOHCH2CH2COOHNO N N=CHCOOHCH3NO N NHCOCH3HNO OHNH2NH2H2NNHCOCH3H3CNHNHCOCH3 HONHNHCOCH3 CH3CO肼 异烟酸N-乙酰异烟肼乙酰肼双乙酰肼 乙酰自由基A Free sample background from Slide 10异烟肼的理化性质异烟肼可与铜离子、铁离子、锌离子等金属离子络合，如与铜离子在酸性条件下生成一分子螯合物，呈红色，在pH7.5时，生成两分子螯合物 NNCu+ON H2NNON H2H2NNCuON
