【摘要】 <正> 缩氨基硫脲类化合物有抗肿瘤、抗病毒和抗菌等多种药理活性。Barret等首次报道了乙二醛二缩氨基硫脲(Ⅰ)的抗疟活性。Klayman等研究了缩更多还原

【Abstract】 A series of 2-formyl （acetyl） substituted quinoline thiosemicarbazones（Ⅲ, ⅩⅡ, ⅩⅢ） were prepared in order to evaluate their antimalarial activity. Oxidation of substituted quinolines （Ⅳ） with selenium dioxide gave 2-formyl substituted quinolines（Ⅴ）. 2-Acetyl substituted quinoline （Ⅸ） was obtained from Ⅳ by oxidation, esterification, Claisen condensation and decarboxylation. Ⅲ_1～9 were synthesized by two methods; one was by condensation of 2-formyl （acetyl） substituted quinolines with methyl hydrazinecarbodithioat to form methyl - 3- [1-（2, quinolinyl） - alkylidene] hydrazinecarbodithioate （ⅩⅠ）, then the S-methyl group of ⅩⅠ was displaced by substituted amines to formthe desired substituted thiosemicarbazones. The other was by condensation of 2-formyl （acetyl） substituted quinolines with 4-substituted-3-thiosemicarbazide （Ⅹ） to afford directly Ⅲ_1～9, Ⅲ_10～12 were obtained by selective reduction of corresponding nitro compounds with stannous chloride and ⅩⅡ as a by-product was obtained by the nonselective reduction of Ⅲ₇ with stannous chloride. 3 - Hexyl - 4 - oxothiazolin - 2 - yl （2 - formyl or acetyl substituted quinoline） hydrazones (ⅩⅢ_1,2) were prepared from Ⅲ_1,4 via cyclization under sodium acetate condition.Eighteen compounds were found to be inactive in mice infected with ANKA strain of Plasmodium berghei.更多还原