UMYMFOR (CONICET-UBA) and Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, 1428 Buenos Aires, Argentina.
Steroids. 2011 Sep-Oct;76(10-11):1160-5. doi: 10.1016/j.steroids.2011.05.005. Epub 2011 May 27.
Disodium 2β,3α-dihydroxy-5α-cholestan-6-one disulfate (8) has been synthesized using cholesterol (1) as starting material. Sulfation was performed using trimethylamine-sulfur trioxide complex in dimethylformamide as the sulfating agent. The acetylcholinesterase inhibitory activity of compound 8 was evaluated and compared to that of disodium 2β,3α-dihydroxy-5α-cholestane disulfate (10) and diols 7 and 9. Compounds 8 and 10 were active with IC(50) values of 14.59 and 59.65 μM, respectively. Diols 7 and 9 showed no inhibitory activity (IC(50)>500 μM).
已使用胆固醇（1）作为起始原料合成了二钠 2β,3α-二羟基-5α-胆甾烷-6-酮二硫酸盐（8）。使用三甲胺-三氧化硫复合物在二甲基甲酰胺中作为磺化剂进行磺化。评估了化合物 8 的乙酰胆碱酯酶抑制活性，并与二钠 2β,3α-二羟基-5α-胆甾烷二硫酸盐（10）和二醇 7 和 9 进行了比较。化合物 8 和 10 的活性具有 IC50 值分别为 14.59 和 59.65 μM。二醇 7 和 9 没有显示抑制活性（IC50>500 μM）。
