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• W2313916324 abstract "The synthesis, structure-activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. The use of structure-guided drug design techniques provided compounds that demonstrated excellent FLAP binding potency (IC50 < 10 nM) and potent inhibition of LTB4 synthesis in human whole blood (IC50 < 100 nM). Optimization of binding and functional potencies, as well as physicochemical properties resulted in the identification of compound 69 (BI 665915) that demonstrated an excellent cross-species drug metabolism and pharmacokinetics (DMPK) profile and was predicted to have low human clearance. In addition, 69 was predicted to have a low risk for potential drug-drug interactions due to its cytochrome P450 3A4 profile. In a murine ex vivo whole blood study, 69 demonstrated a linear dose-exposure relationship and a dose-dependent inhibition of LTB4 production." @default.
• W2313916324 created "2016-06-24" @default.
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• W2313916324 date "2015-02-11" @default.
• W2313916324 modified "2023-09-27" @default.
• W2313916324 title "Synthesis, SAR, and Series Evolution of Novel Oxadiazole-Containing 5-Lipoxygenase Activating Protein Inhibitors: Discovery of 2-[4-(3-{(<i>R</i>)-1-[4-(2-Amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-<i>N</i>,<i>N</i>-dimethyl-acetamide (BI 665915)" @default.
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• W2313916324 doi "https://doi.org/10.1021/jm501185j" @default.
• W2313916324 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25671290" @default.
• W2313916324 hasPublicationYear "2015" @default.
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