2-芳亚胺基-4-噻唑烷酮类化合物的合成及生物活性

目的设计、合成新的2-芳亚胺基-4-噻唑烷酮类化合物并研究其对一氧化氮合酶(NOS)的抑制活性。方法运用N-氯乙酰-1,2,3,4-四氢异喹啉或N-氯乙酰邻苯二甲酰亚胺与取代硫脲反应，简便地合成了15个新的2-芳亚胺基-4-噻唑烷酮类化合物，测试新合成的目标化合物的NOS抑制活性。结果和结论合成了15个新的2-芳亚胺基-4-噻唑烷酮类化合物，大部分反应收率大于65%。所有化合物的结构用¹H NMR，IR，MS及元素分析进行了表征。初步药理筛选结果表明，部分化合物具有NOS抑制活性。

Synthesis and bioactivity of 2-arylimino-4-thiazolidones

Aim To synthesize a series of 2-arylimino-4-thiazolidone derivatives and 2-imidazolino-4-thiazolidone in order to get some novel potent compounds with nitric oxide synthases(NOS) inhibitory activity.Methods The target compounds were prepared by reaction of N-chloroacetyl-1,2,3,4-tetrahydroisoquinoline or N-chloroacetylphthalimide with substituted thioureas,their NOS inhibitory activity were measured.Results and Conclusion The 15 new compounds were synthesized and most of the reaction yields were over 65%.The structures of new compounds were identified by IR,~ 1H NMR,MS and elemental analyses.Bioassay indicated that,most of 15 new compounds synthesized had confirmed bioactivities inhibition against NOS.