| Title : Synthesis and structure-activity relationships for some novel diflapolin derivatives with benzimidazole subunit - Vieider_2022_J.Enzyme.Inhib.Med.Chem_37_1752 |
| Author(s) : Vieider L , Zoeller E , Romp E , Schoenthaler M , Hernandez-Olmos V , Temml V , Hasenoehrl T , Schuster D , Werz O , Garscha U , Matuszczak B |
| Ref : J Enzyme Inhib Med Chem , 37 :1752 , 2022 |
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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. |
| PubMedSearch : Vieider_2022_J.Enzyme.Inhib.Med.Chem_37_1752 |
| PubMedID: 36124840 |
Vieider L, Zoeller E, Romp E, Schoenthaler M, Hernandez-Olmos V, Temml V, Hasenoehrl T, Schuster D, Werz O, Garscha U, Matuszczak B (2022)
Synthesis and structure-activity relationships for some novel diflapolin derivatives with benzimidazole subunit
J Enzyme Inhib Med Chem
37 :1752
Vieider L, Zoeller E, Romp E, Schoenthaler M, Hernandez-Olmos V, Temml V, Hasenoehrl T, Schuster D, Werz O, Garscha U, Matuszczak B (2022)
J Enzyme Inhib Med Chem
37 :1752