کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1371006 | 981834 | 2011 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life](/preview/png/1371006.png)
The continued optimization of a series of glucokinase activators is described, including attempts to understand the interplay between molecular structure and the composite parameter of unbound clearance. These studies resulted in the discovery of a new scaffold for glucokinase activators and further exploration of this scaffold led to the identification of GKA60. GKA60 maintains an excellent balance of potency and physical properties whilst possessing a significantly different, but complimentary, pre-clinical pharmacokinetic profile compared with the previously disclosed compound GKA50.
The continued discovery of a novel series of pyridine acid containing glucokinase activators is described. The composite parameter of unbound clearance was used to aid in the identification of GKA60, a potent, soluble glucokinase activator with excellent bioavailability and increased half-life.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 11, 1 June 2011, Pages 3467–3470