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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
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。 |
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