Article ID Journal Published Year Pages File Type
1367658 Bioorganic & Medicinal Chemistry Letters 2006 6 Pages PDF
Abstract

A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB1-R antagonists and inverse agonists. Optimization of the structure–activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identification of two compounds with oral activity in rodent feeding models (2h and 4a). Replacement of the PP group in 2h with other bicyclic groups resulted in a loss of binding affinity.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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