Design, synthesis and in vitro/in vivo evaluation of orally bioavailable prodrugs of a catechol- O-methyltransferase inhibitor

Compound 1 is an investigational, nanomolar inhibitor of catechol- O-methyltransferase (COMT) that suffers from poor oral bioavailability, most probably due to its low lipophilicity throughout most of the gastrointestinal tract and, to a lesser extent, its rapid systemic clearance. Several lipophili...

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