Synthesis and Structure–activity Relationships for Some Novel Diflapolin Derivatives with Benzimidazole Subunit
Journal of enzyme inhibition and medicinal chemistry(2022)
Abstract
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.
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Key words
Diflapolin,benzimidazoles,soluble epoxide hydrolase (sEH),5-lipoxygenase activating protein (FLAP),solubility and GI absorption prediction
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