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Synthesis and structure-activity relationships for some novel diflapolin derivatives with benzimidazole subunit

A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesised, and characterised. These novel compounds, which contain a benzimidazole subunit were evaluated for their inhibitory activity against sEH...

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Main Authors: Lisa Vieider (Author), Eva Zoeller (Author), Erik Romp (Author), Martin Schoenthaler (Author), Victor Hernández-Olmos (Author), Veronika Temml (Author), Thomas Hasenoehrl (Author), Daniela Schuster (Author), Oliver Werz (Author), Ulrike Garscha (Author), Barbara Matuszczak (Author)
Format: Book
Published: Taylor & Francis Group, 2022-12-01T00:00:00Z.
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Summary:A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesised, and characterised. These novel compounds, which contain a benzimidazole subunit were evaluated for their inhibitory activity against sEH and FLAP. Molecular modelling tools were applied to analyse structure-activity relationships (SAR) on both targets and to predict solubility and gastrointestinal (GI) absorption. The most promising dual inhibitors of these series are 5a, 6b, and 6c.
Item Description:10.1080/14756366.2022.2087645
1475-6374
1475-6366

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