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2-吲哚甲酰肼与取代基为H,CH_3,ClCH_2,C_2H_5,CH_3(CH_2)_3,4-Br-C_6H_4和3-吡啶基的甲酰氯在DMF中反应时均得双酰肼化合物。但在乙腈中与乙酰氯或丙酰氯反应时,分别得到两种失水产物,经~(13)C核磁共振仪分析表明其为吲哚2位(口恶)二唑取代的化合物,其余仍为双酰肼化合物。体外试验显示;N-甲酰基,N-氯代乙酰基-2-吲哚甲酰肼(Ⅰ,Ⅲ)和2-[2-(5-乙基)-1,3,4-(口恶)二唑]-吲哚(Ⅸ)对强毒人型结核菌H_(37)RV有抑制作用。
The diacylhydrazide compounds are obtained when 2-indolylhydrazide is reacted with formyl chloride whose substituents are H, CH_3, ClCH_2, C_2H_5, CH_3 (CH_2) _3,4-Br-C_6H_4 and 3-pyridyl in DMF. However, two kinds of dehydration products were obtained when reacted with acetyl chloride or propionyl chloride in acetonitrile, respectively. The results of 13 C nuclear magnetic resonance spectroscopy showed that it was a compound substituted with oxadiazole (2-oxazoles) Is a bis-hydrazide compound. In vitro tests showed that N-formyl, N-chloroacetyl-2-indolylhydrazide (Ⅰ, Ⅲ) and 2- [2- (5-ethyl) ) Oxadiazole] -indole (Ⅸ) inhibits the virulent Mycobacterium tuberculosis H_ (37) RV.