2-苯基吡唑并[1,5-a]嘧啶-3-基乙酰胺作为外周苯二氮䓬受体配体的研究：合成、生物学评价及三维定量构效关系研究
Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: synthesis, biological evaluation and 3D-QSAR investigation.
作者信息
Selleri Silvia, Gratteri Paola, Costagli Camilla, Bonaccini Claudia, Costanzo Annarella, Melani Fabrizio, Guerrini Gabriella, Ciciani Giovanna, Costa Barbara, Spinetti Francesca, Martini Claudia, Bruni Fabrizio
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via U. Schiff, 6, 50019 Sesto F.no Firenze, Italy.
出版信息
Bioorg Med Chem. 2005 Aug 15;13(16):4821-34. doi: 10.1016/j.bmc.2005.05.015.
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 their ability to modulate the steroid biosynthesis in C6 glioma cells.
本文报道了新型2-苯基吡唑并[1,5-a]嘧啶-3-基乙酰胺作为选择性外周苯二氮䓬受体（PBR）配体的合成及结合研究。研究了3-位取代基的变化情况，并提出了一个3D-QSAR模型来评估不同取代基对乙酰胺部分的影响。此外，还测试了对PBR具有高亲和力的一部分新型化合物调节C6胶质瘤细胞中类固醇生物合成的能力。
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