TY  - JOUR
A1  - Vieider, Lisa
A1  - Romp, Erik
A1  - Temml, Veronika
A1  - Fischer, Jana
A1  - Kretzer, Christian
A1  - Schönthaler, Martin
A1  - Taha, Abdulla
A1  - Hernández-Olmos, Victor
A1  - Sturm, Sonja
A1  - Schuster, Daniela
A1  - Werz, Oliver
A1  - Garscha, Ulrike
A1  - Matuszczak, Barbara
T1  - Synthesis, biological evaluation and structure–activity relationships of diflapolin analogues as dual sEH/FLAP inhibitors
T2  - ACS medicinal chemistry letters
N2  - 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.
KW  - Soluble epoxide hydrolase (sEH)
KW  - 5-Lipoxygenase activating protein (FLAP)
KW  - Arachidonic acid cascade
KW  - Diflapolin
KW  - Inflammation
Y1  - 2018
UR  - http://publikationen.ub.uni-frankfurt.de/frontdoor/index/index/docId/48843
UR  - https://nbn-resolving.org/urn:nbn:de:hebis:30:3-488432
SN  - 1948-5875
N1  - ACS AuthorChoice - This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
VL  - 10
IS  - 1
SP  - 62
EP  - 66
PB  - ACS
CY  - Washington, DC
ER  -