Journal of Medicinal Chemistry p. 10124 - 10143 (2019)
Update date:2022-08-15
Topics:
Adebesin, Adeniyi Michael
Wesser, Tim
Vijaykumar, Jonnalagadda
Konkel, Anne
Paudyal, Mahesh P.
Lossie, Janine
Zhu, Chen
Westphal, Christina
Puli, Narender
Fischer, Robert
Schunck, Wolf-Hagen
Falck, John R.
17(R),18(S)-Epoxyeicosatetraenoic acid (EEQ) is a cytochrome P450 metabolite of eicosapentaenoic acid (EPA) and a powerful negative chronotrope with low nanomolar activity in a neonatal rat cardiomyocyte (NRCM) arrhythmia model. Prior studies identified oxamide 2b as a soluble epoxide hydrolase (sEH) stable replacement but unsuitable for in vivo applications due to limited oral bioavailability and metabolic stability. These ADME limitations have been addressed in an improved generation of negative chronotropes, e.g., 4 and 16, which were evaluated as potential clinical candidates.
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