【摘要】 本文报道带有多巯基的β-巯基乙胺(MEA)和巯基丙胺(MPA)衍生物7,8,9及多巯基酰肼10的合成。由β,β′-(双苄硫基)异丁酸(16)或酯(14)分别经叠氮钠或水合肼作用,可获得化合物17和15,17,15及20经钠-液氨脱苄基,醋酸汞沉淀及硫化氢处理,即得高纯度双巯胺化合物7,10及8。由α,γ-双苄硫基丁胺(12)经同法处理可制得2,4-双巯基-1-氨基对甲苯磺酸盐(9)。这些化合物对小白鼠急性电离辐射损伤均有一定防护作用,其中化合物9具有中等防护效果。更多还原

【Abstract】 In the previous papers we have reported that some tertiary amine derivatives of 1, 2-dithiolane possess protective activity against the lethal effects of ionizing radiation in mice. In the present work, we have continued to prepare some bismercaptoaminoalkanes 7, 8and, 9, and a dimercaptohydrazide 10, which show structural analogy to MEA and APT or 4, and hold promise as radioprotective drugs. These compounds were prepared as follows: The ethyl ester 14 of β, β’-dibenzylmercaptoisobutyric acid (16) reacted with hydrazine to give the corresponding hydrazide 15; 16 via sodium azide reaction was converted to 1, 3-dibenzylmercapto-2-aminopropane hydrochloride (17). α, γ-Dibenzylmercapto-1-aminobutane (12) was prepared similarly from α, γ-dibromobutyryl bromide (11). The debenzylation of 12, 15, 17 and 20 was done with metallic sodium-liquid ammonia and the products were precipitated as mercuric salts, which in turn were treated with hydrogen sulfide in alcohol to yield the pure thiols.Preliminary antiradiation test showed that all the compounds bearing bisthiol function exhibit protective activity in mice. 9 has moderate protective effect against lethal radiation. Details of the pharmacological results will be published elsewhere.更多还原