Title of article
Metabolism investigation leading to novel drug design: Orally active prostacyclin mimetics. Part 4
Author/Authors
Kouji Hattori، نويسنده , , Fujiko Takamura، نويسنده , , Akira Tanaka، نويسنده , , Hisashi Takasugi، نويسنده , , Kiyoshi Taniguchi، نويسنده , , Mie Nishio، نويسنده , , Satoshi Koyama، نويسنده , , Jiro Seki، نويسنده , , Kazuo Sakane، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
3284
To page
3287
Abstract
A metabolism study of FR181157 (1) led to the discovery of new oxazole derivatives as active metabolites. The metabolite 6 with an epoxy ring exhibited high anti-aggregative potency with an IC50 of 5.8 nM and potent binding affinity for the human recombinant IP receptor with a Ki value of 6.1 nM and selectivity for human IP receptor over all other members of the human prostanoid receptor family.
Keywords
Prostacyclin mimetic , Metabolism , IP receptor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795773
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