Movrin M, Medić-Sarić M, Maysinger D, Blazević N
Pharmazie. 1979 Apr;34(4):231-2.
The authors describe the synthesis of I-aminomethylisatin (3) from [I-chloromethylisatin] (1) by means of the Delépine reaction. On condensation with aromatic aldehydes, 3 yields the azomethines 5--7. The azomethine 5 is converted into the corresponding thiosemicarbazone 9. Testing for mitodepressive activity showed that the compounds 5--7 are active. On testing in vitro for tuberculostatic effects, the compound 9 proved exceptionally potent.
作者描述了通过德雷平反应由1-氯甲基异吲哚酮合成1-氨基甲基异吲哚酮(3)的过程。3与芳香醛缩合时生成偶氮甲碱5 - 7。偶氮甲碱5可转化为相应的硫代半卡巴腙9。对有丝分裂抑制活性的测试表明,化合物5 - 7具有活性。在体外进行的抗结核效果测试中,化合物9显示出极强的效力。