| Title : Synthesis, Biological Evaluation and Structure-Activity Relationships of Diflapolin Analogues as Dual sEH\/FLAP Inhibitors - Vieider_2019_ACS.Med.Chem.Lett_10_62 |
| Author(s) : 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 |
| Ref : ACS Med Chem Lett , 10 :62 , 2019 |
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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, 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. |
| PubMedSearch : Vieider_2019_ACS.Med.Chem.Lett_10_62 |
| PubMedID: 30655948 |
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 (2019)
Synthesis, Biological Evaluation and Structure-Activity Relationships of Diflapolin Analogues as Dual sEH\/FLAP Inhibitors
ACS Med Chem Lett
10 :62
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 (2019)
ACS Med Chem Lett
10 :62