Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 1, Pages 62-66Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00415
Keywords
Soluble epoxide hydrolase (sEH); 5-Lipoxygenase activating protein (FLAP); Arachidonic acid cascade; Diflapolin; Inflammation
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Funding
- German Research Council [SFB1278 Polytarget, GA 2101/2-1]
- University of Innsbruck (Doktoratsstipendium der Nachwuchsforderung)
- Austrian Science Fund (FWF) [T942-B30]
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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 H-1 NMR, C-13 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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