Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370089 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
Abstract
Two new series of EP4 antagonists containing a 3-methylaryl-2-carbonyl core have been identified. One series has a 3-substituted-phenyl core, while the other one incorporates a 3-substituted pyridine. Both series led to compounds with potent activity in functional and human whole blood (hWB) assays. In the pyridine series, compound 7a was found to be a highly potent and selective EP4 antagonist, with suitable rat and dog pharmacokinetic profiles.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Maria-Jesus Blanco, Tatiana Vetman, Srinivasan Chandrasekhar, Matthew J. Fisher, Anita Harvey, Mark Chambers, Chaohua Lin, Daniel Mudra, Jennifer Oskins, Xu-Shan Wang, Xiao-Peng Yu, Alan M. Warshawsky,