Discovery of substituted phenyl urea derivatives as novel long-acting β 2-adrenoreceptor agonists

…, A Gavaldá, M Gómez-Angelats, M Miralpeix…

文献索引：Perez, Daniel; Crespo, Maribel; Sole, Laia; Prat, Maria; Carcasona, Carla; Calama, Elena; Otal, Raquel; Gavalda, Amadeu; Gomez-Angelats, Mireia; Miralpeix, Montserrat; Puig, Carles Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 5 p. 1545 - 1548

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被引用次数: 8

摘要

The synthesis of diverse functionalized ureas in a semi-parallel fashion is described, as well as their β1/β2-adrenergic activities and the corresponding structure–activity relationship (SAR). We have focused on lipophilicity and duration of action, and we have discovered a strong correlation in this series of molecules. A quantitative structure–activity relationship (QSAR) analysis will be presented that quantifies this relationship.