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Discovery and optimization of oxadiazole-based FLAP inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-09-08 , DOI: 10.1016/j.bmcl.2017.09.007
Alessandra Bartolozzi , Asitha Abeywardane , Todd Bosanac , John A. Broadwater , Zhidong Chen , J. Matthew Hutzler , John D. Huber , Peter Nemoto , Alan Olague , Doris Riether , Tom Simpson , Hidenori Takahashi , Lifen Wu , Yunlong Zhang , Renee M. Zindell

Structure activity relationship (SAR) investigation of an oxadiazole based series led to the discovery of several potent FLAP inhibitors. Lead optimization focused on achieving functional activity while improving physiochemical properties and reducing hERG inhibition. Several compounds with favorable in vitro and in vivo properties were identified that were suitable for advanced profiling.



中文翻译:

基于二恶唑的FLAP抑制剂的发现和优化

基于恶二唑的系列的结构活性关系(SAR)研究导致发现了几种有效的FLAP抑制剂。铅优化的重点是实现功能活性,同时改善其理化特性并减少hERG抑制作用。鉴定了几种具有良好的体外和体内特性的化合物,适用于高级分析。

更新日期:2017-09-08
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