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liugy2009金蟲 (小有名氣)
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We note two strategic attributes of this work. First, the choice of testing venue for these libraries, although broad, was nonetheless informed by the reported activities of the naturally occurring alkaloids (i.e., it was reasonable to expect that purported antitussive compounds might exert effects on GPCRs found in the CNS). Second, the presence of total syntheses of the natural products themselves as well as versatile, flexible synthetic methods that would allow preparation of a diverse set of analogues was extremely helpful. In the present example, strongly potent ligands ultimately depended on the availability of a secondgeneration synthetic method able to provide a second major scaffold. Overall, this work demonstrates the positive synergy between the activities of natural product synthesis, synthetic methodology, and biological evaluation. |
至尊木蟲 (職業(yè)作家)
至尊木蟲 (職業(yè)作家)
| We note two strategic attributes of this work.我們注意到屬于此項(xiàng)研究的兩種策略。 First, the choice of testing venue for these libraries, although broad, was nonetheless informed by the reported activities of the naturally occurring alkaloids (i.e., it was reasonable to expect that purported antitussive compounds might exert effects on GPCRs found in the CNS). 其一,盡管對這些文庫進(jìn)行測試的選擇比較寬泛,但有天然存在生物堿活性報(bào)道的資料可供借鑒(即就是說,有理由預(yù)期聲稱的鎮(zhèn)咳劑可能對中樞神經(jīng)系統(tǒng)中的GPCR發(fā)揮效應(yīng))。Second, the presence of total syntheses of the natural products themselves as well as versatile, flexible synthetic methods that would allow preparation of a diverse set of analogues was extremely helpful. 其二,天然產(chǎn)物自身的全合成方法和多用途的靈活合成方法十分有利于制備多種多樣系列類似物。In the present example, strongly potent ligands ultimately depended on the availability of a second generation synthetic method able to provide a second major scaffold.在當(dāng)前的例子中, 高效配體從根本上依賴于能夠提供附加重要支架的第二代合成方法。Overall, this work demonstrates the positive synergy between the activities of natural product synthesis, synthetic methodology, and biological evaluation.總體而言,這一研究工作證明天然產(chǎn)物合成活動和合成方法學(xué)與生物學(xué)評價之間值得肯定的協(xié)同作用。 |
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