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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.[1]

References

  1. Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6. Tanaka, A., Hattori, K., Taniguchi, K., Okitsu, O., Tabuchi, S., Nishio, M., Nagakura, Y., Maeda, N., Murai, H., Seki, J. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
 
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