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Synthesis and bioactivity of 2-arylimino-4-thiazolidones
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 9
- DOI:
- 10.3321/j.issn:0513-4870.2006.09.005
- Key Word:
- 4-噻唑烷酮;异硫脲;NOS抑制剂;生物活性
Abstract： 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.
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