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Biotransformation of Prasugrel, a Novel Thienopyridine Antiplatelet Agent, to the Pharmacologically Active Metabolite
TLDR
One possible mechanism for the ultimate formation of R-138727 in vitro can be through formation of a sulfenic acid mediated by P450s followed possibly by a glutathione conjugation to a mixed disulfide and reduction of the disulfides to the active metabolite R- 138727.
Discovery of DS79182026: A potent orally active hepcidin production inhibitor.
[2-(omega-phenylalkyl)phenoxy]alkylamines.II: Synthesis and selective serotonin-2 receptor binding.
TLDR
(S)-2-[2- [2-(3-methoxyphenyl)ethyl]phenoxy]ethyl]-1-methylpyrrolidine, (S)-27, exhibited the most potent and selective affinity for 5-HT2 receptors and was effective in inhibiting 5- HT2-induced vasoconstriction in vitro and platelet aggregation both in vivo and ex vivo.
Cinnamylindoline derivatives: synthesis and factor Xa (FXa) inhibitory activities.
TLDR
Some novel derivatives of cinnamylindoline derivatives showed potent FXa inhibitory activities and good selectivity over trypsin and exhibited potent anticoagulant activities in vitro.
[2-(O-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding (2).
A series of 12-(2-phenylethyl)phenoxy]ethylpyrrolidine derivatives were synthesized, and their affinity for serotonin-2 (5-HT2) and dopamine-2 (D2) receptors was examined. Among them, compound 17,
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