Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374915 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
We have developed a pharmacophore model for the EP3 receptor antagonists based on its endogenous ligand PGE2. This ligand-based design yielded a series of novel peri-substituted [4.3.0] bicyclic aromatics featuring 1-alklyaryl 7-heterocyclic sulfonamide substituents. The synthesized molecules are potent antagonists of human EP3 receptor in vitro and show inhibition of rat platelets aggregation. Optimized derivatives display high selectivity over IP, FP, and other EP receptor panels.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Georgeta Hategan, Alexandre M. Polozov, Wayne Zeller, Hua Cao, Rama K. Mishra, Alex S. Kiselyov, Jose Ramirez, Guðrún Halldorsdottir, Ãorkell Andrésson, Mark E. Gurney, Jasbir Singh,