Insight into 2-phenylpyrazolo [1, 5-a] pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: synthesis, biological evaluation and 3D-QSAR …

…, P Gratteri, C Costagli, C Bonaccini, A Costanzo…

文献索引：Selleri, Silvia; Gratteri, Paola; Costagli, Camilla; Bonaccini, Claudia; Costanzo, Annarella; Melani, Fabrizio; Guerrini, Gabriella; Ciciani, Giovanna; Costa, Barbara; Spinetti, Francesca; Martini, Claudia; Bruni, Fabrizio Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 16 p. 4821 - 4834

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被引用次数: 57

摘要

The present paper reports the synthesis and binding studies of new 2-phenylpyrazolo [1, 5- a] pyrimidin-3-yl acetamides as selective Peripheral Benzodiazepine Receptor (PBR) ligands. The variability of substituents at the 3-position was investigated and a 3D-QSAR model was proposed to evaluate the effect of different substitutions on the acetamide moiety. In addition, a subset of the novel compounds showing high affinity for PBR was tested for ...