School of Chemistry, University of Sydney, Sydney, NSW 2006, Australia.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5799-802. doi: 10.1016/j.bmcl.2010.07.135. Epub 2010 Aug 4.
Herein, we report the synthesis of four new phenyl alkyl ether derivatives (7, 9-11) of the pyrazolo[1,5-a]pyrimidine acetamide class, all of which showed high binding affinity and selectivity for the TSPO and, in the case of the propyl, propargyl, and butyl ether derivatives, the ability to increase pregnenolone biosynthesis by 80-175% over baseline in rat C6 glioma cells. While these compounds fit our in silico generated pharmacophore for TSPO binding the current model does not account for the observed functional activity.
在此，我们报告了吡唑并[1,5-a]嘧啶乙酰胺类的四个新的苯基烷基醚衍生物（7、9-11）的合成，它们都表现出对 TSPO 的高结合亲和力和选择性，并且在丙基、炔丙基和丁基醚衍生物的情况下，能够使大鼠 C6 神经胶质瘤细胞中的 pregnenolone 生物合成增加 80-175%。虽然这些化合物符合我们为 TSPO 结合生成的基于计算机的药效团模型，但当前的模型无法解释观察到的功能活性。
