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

F Takamura, A Tanaka, H Takasugi, K Taniguchi…

文献索引：Takamura, Fujiko; Tanaka, Akira; Takasugi, Hisashi; Taniguchi, Kiyoshi; Nishio, Mie; Seki, Jiro; Hattori, Kouji Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 17 p. 4475 - 4478

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被引用次数: 7

摘要

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 PGI2 mimetics based on blocking the main metabolic pathway of FK788. The new compound 7c was found to be equipotent to FK788 towards PGI2 agonist activity and metabolically more stable than FK788.