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烟云听雨铁杆木虫 (正式写手)
金虫
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[求助]
求翻译一段英文文献（药化）
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Next, a total of 104 synthetic Stemona analogues were selected for screening as described above [Fig. 3; for the complete binding data (numeric κi values) and compound identity, see Dataset S1]. The entries in Fig. 3 are grouped according to compound class as indicated in Scheme 2. Several patterns become discernable when analyzed from this perspective. The reductive amination compounds, derived primarily from aryl-containing amines, tended to possess hit profiles against the GPCR panel of greater potency and lower selectivity than most other compound classes. Similar trends of potency and selectivity were observed for the indole compound set. The Friedländer quinoline analogues displayed a more balanced activity/selectivity profile, whereas the carbamate analogue compound set, which lacks any basic nitrogen, demonstrated more modest binding activity. The results obtained for the twelve representative analogues displayed in Fig. 4 demonstrate these trends. Although compounds possessing submicromolar affinities for multiple classes of GPCR targets (e.g., adrenergic, muscarinic, serotonin, dopaminergic and Sig-R classes) emerged as possible hits for further investigation, we were most interested in a clustering of basic, nitrogencontaining compounds displaying potent affinity for the Sig-Rs (compounds 6{1–3, 8, and 9}). Of secondary interest was the adrenergic binding of the tertiary amines derived from the amide reduction of the core scaffolds. Thus, 6{10} possessed analpha1D Ki of 18 nM with no additional binding of <10;000 nM,and 6{11} possessed an alpha1D Ki of 208 nM and a sigma2 Ki of 5,970 nM. |
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【答案】应助回帖
烟云听雨(金币+35, 翻译EPI+1): 谢谢 2011-06-09 23:25:01
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Next, a total of 104 synthetic Stemona analogues were selected for screening as described above [Fig. 3; for the complete binding data (numeric κi values) and compound identity, see Dataset S1]. 接着，共有104种合成的百部类似物可供如上所述的筛选【图3；这样做也是为了完成绑定数据（数值ki值）及化合物的种类鉴定，见S1数据集】 The entries in Fig. 3 are grouped according to compound class as indicated in Scheme 2. 图3中的条目是依据表2中显示的化合物类来分组的。 Several patterns become discernable when analyzed from this perspective. 从以上这个角度分析可知，这几种模式是有迹可寻的。 The reductive amination compounds, derived primarily from aryl-containing amines, tended to possess hit profiles against the GPCR panel of greater potency and lower selectivity than most other compound classes. 主要是从芳环胺类化合物中衍生的胺类化合物的还原，往往具有依靠有更大效能的G蛋白偶联受体的概况，以及比大多数其他化合物类更低的选择性。 Similar trends of potency and selectivity were observed for the indole compound set. 类似的效能和选择性趋势在吲哚类化合物中也能够观察到。 The Friedländer quinoline analogues displayed a more balanced activity/ selectivity profile, whereas the carbamate analogue compound set, which lacks any basic nitrogen, demonstrated more modest binding activity. Friedlä指出，喹啉类似物表现出更加平衡的活性/选择性，而氨基甲酸酯类化合物，因为缺乏基氮，而表现出更加温和的结合活性。 The results obtained for the twelve representative analogues displayed in Fig. 4 demonstrate these trends. 图4中的12个代表性的类似物的结果显示了这种趋势。 Although compounds possessing submicromolar affinities for multiple classes of GPCR targets (e.g., adrenergic, muscarinic, serotonin, dopaminergic and Sig-R classes) emerged as possible hits for further investigation, we were most interested in a clustering of basic, nitrogencontaining compounds displaying potent affinity for the Sig-Rs (compounds 6{1–3, 8, and 9}). 虽然由于有多类型的G蛋白偶联受体目标物（如肾上腺素，胆碱，血清素，多巴胺以及Sig-R类）而使得化合物的亲和力较低，但这种情况的出现对于进一步的调查访问也是有力的。 我们最感兴趣的聚类基本物，含氮类化合物在Sig- R上显示出强大的亲和力（化合物6{1-3，8，9}）。 Of secondary interest was the adrenergic binding of the tertiary amines derived from the amide reduction of the core scaffolds. 酰胺还原的衍生物如三级胺，其与肾上腺素受体的结合也是我们接着需要研究的。 |
2楼2011-06-09 21:10:07