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煙云聽雨

鐵桿木蟲 (正式寫手)

金蟲

應(yīng)助: 3 (幼兒園)
金幣: 8375.9
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帖子: 482
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[求助] 求翻譯一段英文文獻(xiàn)（藥化）

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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1樓 2011-06-07 17:54:54

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rongfang

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【答案】應(yīng)助回帖

煙云聽雨(金幣+35, 翻譯EPI+1): 謝謝 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].
接著，共有104種合成的百部類似物可供如上所述的篩選【圖3；這樣做也是為了完成綁定數(shù)據(jù)（數(shù)值ki值）及化合物的種類鑒定，見S1數(shù)據(jù)集】
The entries in Fig. 3 are grouped according to compound class as indicated in Scheme 2.
圖3中的條目是依據(jù)表2中顯示的化合物類來分組的。
Several patterns become discernable when analyzed from this perspective.
從以上這個角度分析可知，這幾種模式是有跡可尋的。
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.
主要是從芳環(huán)胺類化合物中衍生的胺類化合物的還原，往往具有依靠有更大效能的G蛋白偶聯(lián)受體的概況，以及比大多數(shù)其他化合物類更低的選擇性。
Similar trends of potency and selectivity were observed for the indole compound set. 類似的效能和選擇性趨勢在吲哚類化合物中也能夠觀察到。
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，喹啉類似物表現(xiàn)出更加平衡的活性/選擇性，而氨基甲酸酯類化合物，因為缺乏基氮，而表現(xiàn)出更加溫和的結(jié)合活性。
The results obtained for the twelve representative analogues displayed in Fig. 4 demonstrate these trends.
圖4中的12個代表性的類似物的結(jié)果顯示了這種趨勢。
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}).
雖然由于有多類型的G蛋白偶聯(lián)受體目標(biāo)物（如腎上腺素，膽堿，血清素，多巴胺以及Sig-R類）而使得化合物的親和力較低，但這種情況的出現(xiàn)對于進(jìn)一步的調(diào)查訪問也是有力的。我們最感興趣的聚類基本物，含氮類化合物在Sig- R上顯示出強(qiáng)大的親和力（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.
酰胺還原的衍生物如三級胺，其與腎上腺素受體的結(jié)合也是我們接著需要研究的。

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2樓2011-06-09 21:10:07