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ID: ALA1140242
Journal: Bioorg Med Chem Lett
Title: Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
Authors: Hattori K, Takamura F, Tanaka A, Takasugi H, Taniguchi K, Nishio M, Koyama S, Seki J, Sakane K.
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 IC(50) of 5.8 nM and potent binding affinity for the human recombinant IP receptor with a K(i) value of 6.1 nM and selectivity for human IP receptor over all other members of the human prostanoid receptor family.
CiteXplore: 15935659