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目的:合成2-(4’-甲基氨基苯)-6-羟基苯并噻唑(6-OH-BTA-1,也称PIB),并进行~3H标记得到[~3H]6-CH_3O-BTA-Me,评价其生物活性和应用价值。方法:对PIB前体6-OH-BTA-0的合成方法进行优化改进,使用氢碘酸经一步反应由化合物4得到6-OH-BTA-0,继续和碘甲烷反应得到6-OH-BTA-1,6-OH-BTA-1与氚标记的碘甲烷反应制备[~3H]6-CH_3O-BTA-Me,在体外测定6-OH-BTA-0和6-OH-BTA-1与AD患者脑匀浆组织的亲和性。结果:所有化合物结构得到确证,6-OH-BTA-0和6-OH-BTA-1的Ki值分别为33.5 nmol·L~(-1)和8.8 nmol·L~(-1),表明与Aβ具有良好的亲和性。结论:自制的PIB可以用于AD的早期诊断实验研究。
OBJECTIVE: To synthesize 2- (4’-methylaminobenzene) -6-hydroxybenzothiazole (6-OH-BTA-1, also called PIB) -Me, evaluate its biological activity and application value. Methods: The synthesis of PIB precursor 6-OH-BTA-0 was optimized and improved. 6-OH-BTA-0 was obtained from compound 4 by one step reaction with hydroiodic acid and then reacted with methyl iodide to obtain 6-OH-BTA 6-OH-BTA-1 was reacted with tritiated iodomethane to prepare [~ 3H] 6-CH 3 O-BTA-Me. Patient brain homogenate tissue affinity. Results: The structures of all the compounds were confirmed. The Ki values of 6-OH-BTA-0 and 6-OH-BTA-1 were 33.5 nmol·L -1 and 8.8 nmol·L -1, Aβ has good affinity. Conclusion: Homemade PIB can be used in the early diagnosis of AD.