Discovery and optimization of oxadiazole-based FLAP inhibitors.

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

Bioorganic & Medicinal Chemistry Letters（2017）

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摘要

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.

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关键词

FLAP,5-Lipoxygenase activating protein,Leukotrienes,Cardiovascular diseases,Oxadiazole,Solubility,hERG

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