Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: Orally active prostacyclin mimetics. Part 6

The synthesis and biological activity of novel derivatives of our previously reported IP receptor agonist FR181157 is described. SAR studies to replace the cyclohexene-linker of FR181157 led to the discovery of compound 1i (FR207845) as a potent non-prostanoid PGI2 mimetic with good oral bioavailability.

Graphical abstractThe synthesis and biological activity of novel derivatives of our previously reported IP receptor agonist FR181157, replacing the cyclohexene-linker, is described. Compound 1i (FR207845) was identified as a potent non-prostanoid PGI2 mimetic with a good oral bioavailability.Figure optionsDownload full-size imageDownload as PowerPoint slide