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ID: ALA4043239

Journal: Bioorg Med Chem Lett

Title: Discovery and optimization of oxadiazole-based FLAP inhibitors.

Authors: Bartolozzi A, Abeywardane A, Bosanac T, Broadwater JA, Chen Z, Hutzler JM, Huber JD, Nemoto P, Olague A, Riether D, Simpson T, Takahashi H, Wu L, Zhang Y, Zindell RM.

Abstract: 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.

CiteXplore: 28927794

DOI: 10.1016/j.bmcl.2017.09.007