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

[Image: see text] 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 (1)H NMR, (13)C NMR, and elemental analysis. These novel compounds were biologically evaluated fo...

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Detalles Bibliográficos
Autores principales: Vieider, Lisa, Romp, Erik, Temml, Veronika, Fischer, Jana, Kretzer, Christian, Schoenthaler, Martin, Taha, Abdulla, Hernández-Olmos, Victor, Sturm, Sonja, Schuster, Daniela, Werz, Oliver, Garscha, Ulrike, Matuszczak, Barbara
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6331193/
https://www.ncbi.nlm.nih.gov/pubmed/30655948
http://dx.doi.org/10.1021/acsmedchemlett.8b00415
Descripción
Sumario:[Image: see text] 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 (1)H NMR, (13)C 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.

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