Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6 |
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| Authors: | Tanaka Akira Hattori Kouji Taniguchi Kiyoshi Okitsu Osamu Tabuchi Seiichiro Nishio Mie Nagakura Yasunori Maeda Noriaki Murai Hidetsugu Seki Jiro |
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| Affiliation: | Chemistry Research Laboratories, Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. akira-tanaka@jp.astellas.com |
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| Abstract: | 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. |
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