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• W2053402936 abstract "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." @default.
• W2053402936 created "2016-06-24" @default.
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• W2053402936 date "2010-04-01" @default.
• W2053402936 modified "2023-10-06" @default.
• W2053402936 title "Design, synthesis and in vitro/in vivo evaluation of orally bioavailable prodrugs of a catechol-O-methyltransferase inhibitor" @default.
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• W2053402936 doi "https://doi.org/10.1016/j.bmcl.2010.02.057" @default.
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