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

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-09, Vol.16 (17), p.4475-4478
Main Authors: Takamura, Fujiko, Tanaka, Akira, Takasugi, Hisashi, Taniguchi, Kiyoshi, Nishio, Mie, Seki, Jiro, Hattori, Kouji
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Biological and medical sciences
Biomimetics
Disease Models, Animal
Drug Design
Epoprostenol - administration & dosage
Epoprostenol - chemistry
Epoprostenol - metabolism
Epoprostenol - pharmacology
FK788
Humans
Liver - drug effects
Liver - injuries
Liver - metabolism
Medical sciences
Metabolism
Microsomes - drug effects
Miscellaneous
Molecular Structure
PGI2
Pharmacology. Drug treatments
Prostacyclin
Rats
Structure-Activity Relationship
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.06.033