期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 10, 页码 2705-2709出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.02.022
关键词
diabetes; glucokinase; kinase activator; unbound clearance; GKA50
The optimisation of a series of glucokinase activators is described, including attempts to uncouple the relationship between potency and plasma protein binding, and to better understand the key pharmacokinetic properties of the series. The use of unbound clearance as an optimisation parameter facilitated the identification of GKA50, a compound which combines excellent potency and pharmacokinetics with good free drug levels and solubility, and exhibits in vivo efficacy at 1 mg/kg po in an acute rat OGTT model. (C) 2006 Elsevier Ltd. All rights reserved.
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