Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries
Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries
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DOI：
10.1021/jo300974j
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发表时间：
2012-09-07
影响因子：
3.6
通讯作者：
Marcaurelle, Lisa A.
中科院分区：
文献类型：
--
作者：
Lowe, Jason T.;Lee, Maurice D.;Marcaurelle, Lisa A.
描述了密集官能化氮杂环丁烷环系统的合成和多样化，以获得各种稠合、桥联和螺环系统。测量代表性库成员的体外物理化学和药代动力学特性，以评估这些支架在生成用于靶向中枢神经系统的先导样分子中的用途。还描述了 1976 元螺环氮杂环丁烷库的固相合成。
The synthesis and diversification of a densely functionalized azetidine ring system to gain access to a wide variety of fused, bridged, and spirocyclic ring systems is described. The in vitro physicochemical and pharmacokinetic properties of representative library members are measured in order to evaluate the use of these scaffolds for the generation of lead-like molecules to be used in targeting the central nervous system. The solid-phase synthesis of a 1976-membered library of spirocyclic azetidines is also described.