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

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

  • Bioorg Med Chem Lett. 2006 Sep 1;16(17):4475-8. doi: 10.1016/j.bmcl.2006.06.033.
Fujiko Takamura 1,  Akira Tanaka,  Hisashi Takasugi,  Kiyoshi Taniguchi,  Mie Nishio,  Jiro Seki,  Kouji Hattori
Affiliations

Affiliation

  • 1 Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Yodogawa-ku, Osaka, Japan.
PMID: 16824754 DOI: 10.1016/j.bmcl.2006.06.033
Abstract

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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