Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379724 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
The new classes of diphenylcarbamate derivatives with a tetrahydronaphthalene skeleton as highly potent and selective IP agonists have been discovered. The optimized diphenylcarbamate type compound FK-788: (R)-4 exhibited potent antiaggregative potency with an IC50 of 18 nM and high binding affinity for the human recombinant IP receptor with Ki values of 20 nM and selectivity for human IP over all other members of the human prostanoid receptor family. Compound (R)-4 was shown to exhibit good pharmacokinetic properties in rats and dogs, and also good bioavailability in healthy volunteers.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kouji Hattori, Akira Tanaka, Osamu Okitsu, Seiichiro Tabuchi, Kiyoshi Taniguchi, Mie Nishio, Satoshi Koyama, Masahide Higaki, Jiro Seki, Kazuo Sakane,