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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. |
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8814402
至尊木虫 (职业作家)
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【答案】应助回帖
★
liugy2009(金币+50, 翻译EPI+1): O(∩_∩)O谢谢~~~ 2011-07-20 19:20:01
Mally89(金币+1): 感谢应助！~ 2011-07-23 22:03:36
liugy2009(金币+50, 翻译EPI+1): O(∩_∩)O谢谢~~~ 2011-07-20 19:20:01
Mally89(金币+1): 感谢应助！~ 2011-07-23 22:03:36
| We note two strategic attributes of this work.我们注意到属于此项研究的两种策略。 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，尽管对这些文库进行测试的选择比较宽泛，但有天然存在生物碱活性报道的资料可供借鉴（即就是说，有理由预期声称的镇咳剂可能对中枢神经系统中的GPCR发挥效应）。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，天然产物自身的全合成方法和多用途的灵活合成方法十分有利于制备多种多样系列类似物。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.在当前的例子中， 高效配体从根本上依赖于能够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.总体而言，这一研究工作证明天然产物合成活动和合成方法学与生物学评价之间值得肯定的协同作用。 |
3楼2011-07-20 10:47:26
8814402
至尊木虫 (职业作家)
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2楼2011-07-20 10:07:08
