Article ID Journal Published Year Pages File Type
1375650 Bioorganic & Medicinal Chemistry Letters 2009 5 Pages PDF
Abstract
A series of peri-substituted [4.3.0] bicyclic non-aromatic heterocycles have been identified as potent and selective hEP3 receptor antagonists. These molecules adopt a hair-pin conformation that overlaps with the endogenous ligand PGE2 and fits into an internally generated EP3 pharmacophore model. Optimized compounds show good metabolic stability and improved solubility over their corresponding bicyclic aromatic analogues.
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
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