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Synthesis, Biological Evaluation and Structure: Activity Relationships of Diflapolin Analogues as Dual sEH/FLAP Inhibitors

: Vieider, L.; Romp, E.; Temml, V.; Fischer, J.; Kretzer, C.; Schoenthaler, M.; Taha, A.; Hernandez-Olmos, V.; Sturm, S.; Schuster, D.; Werz, O.; Garscha, U.; Matuszczak, B.


ACS medicinal chemistry letters 10 (2019), No.1, pp.62-66
ISSN: 1948-5875 (online)
Journal Article
Fraunhofer IME ()

A series of derivatives of the potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor diflapolin was designed, synthesized, and characterized by 1H NMR, 13C NMR, and elemental analysis. These novel compounds were biologically evaluated for their inhibitory activity against sEH and FLAP. Molecular modeling tools were applied to analyze structure–activity relationships (SAR) on both targets. Results show that even small modifications on the lead compound diflapolin markedly influence the inhibitory potential, especially on FLAP, suggesting very narrow SAR.