CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs
复制标题
DOI：
10.1016/j.bmc.2011.08.033
复制
发表时间：
2011-10-01
影响因子：
3.5
通讯作者：
Baker, Bill J.
中科院分区：
文献类型：
--
作者：
Lebar, Matthew D.;Hahn, Kristopher N.;Baker, Bill J.
海洋无脊椎动物来源的黄曲霉素A。最初提出的psammopemmin A的结构。并合成了几种相关的3-嘧啶基吲哚类似物，随后研究了其中枢神经系统、抗疟疾和细胞毒活性。吲哚硼酸酯与嘧啶亲电试剂的Suzuki偶联用于形成天然产物及其衍生物。发现3-嘧啶吲哚可阻止放射性配体与几种CNS受体和转运蛋白结合，最显著的是5-羟色胺受体（
The marine invertebrate-derived meridianin A. the originally proposed structure for psammopemmin A. and several related 3-pyrimidylindole analogs were synthesized and subsequently investigated for central nervous system, antimalarial, and cytotoxic activity. A Suzuki coupling of an indoleborate ester to the pyrimidine electrophile was utilized to form the natural product and derivatives thereof. The 3-pyrimidineindoles were found to prevent radioligand binding to several CNS receptors and transporters, most notably, serotonin receptors (