Synthesis and acetylcholinesterase inhibitory activity of polyhydroxylated sulfated steroids: Structure/activity studies

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• 作者：Victoria Richmond ; Ana P. Murray ; Marta S. Maier
• 关键词：Sulfated steroids ; Synthesis ; Acetylcholinesterase activity
• 刊名：Steroids
• 出版年：2013
• 出版时间：November, 2013
• 年：2013
• 卷：78
• 期：11
• 页码：1141-1147
• 全文大小：700 K

文摘

Disulfated and trisulfated steroids have been synthesized from cholesterol and their acetylcholinesterase inhibitory activity has been evaluated. In our studies we have found that the activity was not only dependent on the location of the sulfate groups but on their configurations. 2¦Â,3¦Á,6¦Á-trihydroxy-5¦Á-cholestan-6-one trisulfate (<strong class=""boldFont"">18strong>) was the most active steroid with an IC<sub>50sub> value of 15.48 ¦ÌM comparable to that of 2¦Â,3¦Á-dihydroxy-5¦Á-cholestan-6-one disulfate (<strong class=""boldFont"">1strong>). Both compounds were found to be less active than the reference compound eserine. The butyrylcholinesterase activity of <strong class=""boldFont"">1strong> and <strong class=""boldFont"">18strong> was one magnitude lower than that against acetylcholinesterase revealing a selective inhibitor profile.