1-烃基(或氢)-3-[4-(5-取代苯并咪(噻)唑-2-巯基)苯基]硫脲的合成及其iNOS抑制活性  

Synthesis and iNOS Inhibitory Activity of 1-Alkyl(or Hydro)-3-[4-(5-Substituted Benzimidazole(or Benzothiazole)-2-Mercapto) Phenyl] Thioureas

作　　者：徐云根[1] 罗穗[1] 华维一[1] 朱东亚[1] 

机构地区：[1]中国药科大学新药研究中心,南京210009

出　　处：《中国药科大学学报》2004年第6期487-490,共4页Journal of China Pharmaceutical University

摘　　要：目的设计和合成出新的硫脲衍生物并研究其对iNOS的抑制活性。方法以2巯基5取代苯并咪(噻)唑(1)为原料,经缩合和还原得到2(4氨基苯硫基)5取代苯并咪(噻)唑(3),3与异硫氰酸苯甲酰酯反应后再水解得到单取代的硫脲(5),或3与异硫氰酸烃基酯反应得到1,3双取代硫脲(6)。按NO试剂盒方法测定了目标化合物的iNOS抑制活性。结果和结论合成了13个未见文献报道的硫脲衍生物,其结构经IR,1HNMR,MS及元素分析确证。初步的药理试验表明,13个目标化合物均有不同程度的iNOS抑制活性,其中化合物6e～6i的iNOS抑制活性强于阳性对照药氨基胍。AIM:To study the synthesis and iNOS inhibitory activity of new thiourea derivatives. METHOD: Substitution,reduction,acylation and hydrolysis were used in the synthesis of the title compounds. The iNOS inhibitory activity of the target compounds was measured based on NO test kit method. RESULT and CONCLUSION:Thirteen compounds of 1-alkyl(or hydro)-3-[4-(5-substituted benzimidazole(or benzothiazole)-2-mercapto) phenyl] thioureas were prepared,and their structures were indentified by IR, 1 H NMR ,MS and EA. The preliminary biological test showed that all of the compounds had the ability to inhibit iNOS,and compounds 6e～6ihad stronger activity than that of the control aminoguanidine.

关 键 词：INOS抑制剂 硫脲 合成 败血性休克 炎症 

分 类 号：TQ463[化学工程—制药化工]