Synthesis of "neoprofen", a rigidified analogue of ibuprofen, exemplifying synthetic methodology for altering the 3-D topology of pharmaceutical substances.
Synthesis of "neoprofen", a rigidified analogue of ibuprofen, exemplifying synthetic methodology for altering the 3-D topology of pharmaceutical substances.
复制标题
“新洛芬”（一种布洛芬的刚性类似物）的合成，举例说明了改变药物物质 3-D 拓扑结构的合成方法。
DOI：
10.1039/c6ob01351a
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发表时间：
2016
影响因子：
3.2
通讯作者：
Dudley,GregoryB
中科院分区：
文献类型：
--
作者：
Ramsubhag,RonR;Massaro,ChelseaL;Dadich,ChristinaM;Janeczek,AndrewJ;Hoang,TungT;Mazzio,ElizabethA;Eyunni,Suresh;Soliman,KaramFA;Dudley,GregoryB
3，3-二甲基环戊烷（新戊烯）在自然界中普遍存在，但在合成药物库中基本上不存在。新戊烯定义了一个疏水和刚性的3-D拓扑结构，具有独特的分子药理学，如这里所示的合成抗炎药物布洛芬的两个新戊烯融合类似物。
3,3-Dimethylcyclopentanes (neopentylenes) are ubiquitous in Nature but largely absent from synthetic pharmaceutical libraries. Neopentylenes define a hydrophobic and rigid 3-D topology with distinct molecular pharmacology, as exemplified here with two neopentylene-fused analogues of the synthetic anti-inflammatory drug, ibuprofen.