1226871-22-2Relevant academic research and scientific papers
Design, synthesis and in vitro/in vivo evaluation of orally bioavailable prodrugs of a catechol-O-methyltransferase inhibitor
Rautio, Jarkko,Lepp?nen, Jukka,Lehtonen, Marko,Laine, Krista,Koskinen, Mikko,Pystynen, Jarmo,Savolainen, Jouko,Sairanen, Mikko
, p. 2614 - 2616 (2010)
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 lipophilic esters were designed as prodrugs and synthesized in an attempt to optimize presystemic drug absorption. A modest twofold increase in 6-h exposure of 1 was observed with two prodrugs, compared to that of 1, after oral treatment in rats.
