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Metabolism investigation leading to novel drug design 2: orally active prostacyclin mimetics. Part 5. | LitMetric

Metabolism investigation leading to novel drug design 2: orally active prostacyclin mimetics. Part 5.

Bioorg Med Chem Lett

Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Yodogawa-ku, Osaka, Japan.

Published: September 2006

A metabolism study of FK788 (2) led to the discovery of new diphenylcarbamoyl derivatives as prostacyclin mimetics without the PG skeleton. We designed and evaluated PGI(2) mimetics based on blocking the main metabolic pathway of FK788. The new compound 7c was found to be equipotent to FK788 towards PGI(2) agonist activity and metabolically more stable than FK788.

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http://dx.doi.org/10.1016/j.bmcl.2006.06.033DOI Listing

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