Discovery and optimization of oxadiazole-based FLAP inhibitors.

Bioorg Med Chem Lett

Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.

Published: October 2017

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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http://dx.doi.org/10.1016/j.bmcl.2017.09.007DOI Listing

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