The use of spirocyclic scaffolds in drug discovery

被引:837
作者
Zheng, Yajun [1 ]
Tice, Colin M. [1 ]
Singh, Suresh B. [1 ]
机构
[1] Vitae Pharmaceut Inc, Ft Washington, PA 19034 USA
关键词
Spirocyclic; Scaffold; Drug discovery; 1; BACE1; INHIBITORS; MACROCYCLIC INHIBITORS; UREA DERIVATIVES; RECEPTOR LIGANDS; INVERSE AGONISTS; POTENT; DESIGN; OPTIMIZATION; BETA; IDENTIFICATION;
D O I
10.1016/j.bmcl.2014.06.081
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Owing to their inherent three-dimensionality and structural novelty, spiro scaffolds have been increasingly utilized in drug discovery. In this brief review, we highlight selected examples from the primary medicinal chemistry literature during the last three years to demonstrate the versatility of spiro scaffolds. With recent progress in synthetic methods providing access to spiro building blocks, spiro scaffolds are likely to be used more frequently in drug discovery. (C) 2014 The Authors. Published by Elsevier Ltd.
引用
收藏
页码:3673 / 3682
页数:10
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