期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 8, 页码 2614-2616出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.057
关键词
Prodrug; COMT inhibitor; Oral bioavailability
资金
- Academy of Finland [132637]
- Academy of Finland (AKA) [132637, 132637] Funding Source: Academy of Finland (AKA)
Compound 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. (C) 2010 Elsevier Ltd. All rights reserved.
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