非甾体抗炎药.pptVIP

5-pyrazolidinonesand3,5-pyrazolidinediones2.3.23,5-吡唑烷二酮类

TDs保泰松(Phenylbutazone):良好的消炎镇痛作用,对胃肠道毒性大,长期服用可损伤肾脏、肝脏、心脏和神经系统,还可引起再和粒细胞缺乏症等;羟布宗(Oxyphenbutazone):具有消炎抗风湿作用,且毒性较低,副作用较小;羟布宗为保泰松的体内代谢产物.Review-ThemechanismofNSAIDsVersusthemechanismofSAIDsReview-StructuraltypesoftheNSAIDSNSAIDSSalicylatesAcetanilidePyrazoleketonesArylalkylacidAnthranilicacids1,2-BenzothiazinesReview-ThestructureandstabilitiesofParacetamolChemicalName:N-(4-hydroxyphenyl)-Acetamide;4-Acetaminophenol;AcetaminophenReview-ThestructureofAspirin:ChemicalName:2-acetoxybenzoicacidThestabilitiesandthepossibleimpuritiesofAspirin.Thesourceofaspirinandthemethodstoidentifythem.3,5-pyrazolidinedionesPhenylbutazoneOxyphenbutazoneAmetaboliteofphenylbutazoneSARofPhenylbutazoneMetabolismofPhenylbutazoneinvivo2.4芳基烷酸类

Arylalkanoicacids芳基烷酸类?芳基乙酸类芳基丙酸类吲哚美辛布洛芬2.4.1芳基乙酸类

Aryl-aceticacids植物生长激素吲哚乙酸,萘乙酸,苯氧乙酸等具有抗炎活性.吲哚美辛,1961(Indomethacin)具有良好的抗炎活性常有胃肠道等副反应炎症介质[TD]-1DiscoveryofIndomethacin典型药物：吲哚美辛Indometacin结构和化学名1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1H-吲哚-3-乙酸1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-aceticacid消炎痛的药理作用强力镇痛消炎药约为Phenylbutazone的25倍解热作用强于Aspirin和Paracetamol镇痛作用为Aspirin的10倍治疗风湿性和类风湿性关节炎等.毒副作用较严重芳基乙酸类非NSAIDs发现5-羟色胺(Serotonin,5HT)为炎症的化学致痛物质Serotonin的体内生物来源与色氨酸(Tryptophan)有关发现风湿患者体内Tryptophan代谢水平较高发现对吲哚乙酸类衍生物进行了研究约300多个吲哚类衍生物中得到Indometacin发现不能拮抗5-HT，不能纠正色氨酸的异常代谢偶然性“消炎痛的出现也并不偶然，不过是我们大量抗炎研究工作的必然酬报罢了”(沈宗瀛先生)Indomethacin的合成Fischerindolesynthesis以对甲氧苯胺为原料SynthesisAnalysisFischerindolesynthesis以对甲氧苯胺为原料FischerindolesynthesisProducesthearomaticheterocycleindolefroma(substituted)phenylhydrazineandanaldehydeorketoneunderacidicconditions.Discoveredin1883byHermannEmilFischer，1902NPReactionMechanismPhysicalProperties吲哚美辛为类白色或微黄色结晶性粉末，室温下在空气中稳定。SPRFGCOOH-CONH-ReactionReactions1.酸性；2.水解性