Synthesis of non-THF analogs of acetogenin toward simplified mimics
Synthesis of non-THF analogs of acetogenin toward simplified mimics
复制标题
DOI：
10.1016/j.tetlet.2005.05.150
复制
发表时间：
2005-08-22
影响因子：
1.8
通讯作者：
Miyoshi, H
中科院分区：
文献类型：
--
作者：
Fujita, D;Ichimaru, N;Miyoshi, H
通过对映体选择性合成1,2-环戊二醇双醚骨架取代双邻THF环，合成醋酸原素类似物，得到简化的模拟物，并检测其对线粒体nadh -泛醌氧化还原酶（复合体I）的抑制作用。结果清楚地表明，1,2-环戊二醇双醚基序可以替代双thf环，同时在纳摩尔水平上保持非常有效的抑制活性。(c) 2005 Elsevier Ltd版权所有。
Acetogenin analogs in which the bis-adjacent THF ring was replaced with an enantioselectively synthesized 1,2-cyclo-pentanediol bis-ether skeleton were synthesized to obtain simplified mimics, and their inhibitory effect on mitochondrial NADH-ubiquinone oxidoreductase (complex I) was examined. The results clearly demonstrate that the 1,2-cyclopentanediol bis-ether motif can substitute for the bis-THF ring while maintaining very potent inhibitory activity at the nanomolar level. (c) 2005 Elsevier Ltd. All rights reserved.