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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Detalles Bibliográficos
Autores principales: Vieider, Lisa, Zoeller, Eva, Romp, Erik, Schoenthaler, Martin, Hernández-Olmos, Victor, Temml, Veronika, Hasenoehrl, Thomas, Schuster, Daniela, Werz, Oliver, Garscha, Ulrike, Matuszczak, Barbara
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2022
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9518245/
https://www.ncbi.nlm.nih.gov/pubmed/36124840
http://dx.doi.org/10.1080/14756366.2022.2087645
Descripción
Sumario: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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