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小木虫论坛-学术科研互动平台» 学术交流区» 论文翻译 » 论文翻译求助完结子版 » 求高手翻译两段 英译汉
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411iloveyo

木虫 (小有名气)

[求助] 求高手翻译两段 英译汉

Three potent Sig-R binding compounds—10{20}, 10{22}, and
10{7} (which contains two basic nitrogen atoms)—were evaluated
for their GPCR selectivity against 38 targets, and the results
were incorporated in Table 1 (see SI Appendix for a heat map–
formatted selectivity table). The three compounds displayed
>86∶1 selectivities for the limited number of receptors for which
binding was observed at all; an impressive result for compounds
obtained in such an abbreviated structure-activity optimization
exercise. The N-propyl derivative 10{22}, designed to eliminate
binding arising from a pendant aryl-containing side chain, was
particularly selective. Here, the only non-Sig-R binding was detected
against the 5HT1A receptor (Ki ¼ 4;500 nM) as opposed
to Sig-R 1 and Sig-R 2 (Ki values of 12 and 288 nM, respectively),
As part of our efforts toward greater skeletal diversity, additional
ring systems were introduced through modifications of
the ketone carbonyl on scaffolds constructed by a Diels–Alder/
Schmidt reaction sequence.We applied the isocyanide multicomponent
reaction (MCR) methodology developed by Shaabani
et al. to transform the ketone carbonyl to the spirocyclic nitrogen
heterocycles shown (Scheme 4) (45). This protocol smoothly
incorporated three elements of diversity in a single operation to
afford 44 heterocyclic analogues synthesized from the fragment
pool in Scheme 4. This chemotype possesses an intriguing, complex
spirocyclic molecular architecture not reported from any
natural sources and incorporating three additional basic nitrogen
sites. Although the MCR was not completely diastereoselective, a
trend we had previously observed in the reductive amination at
the same ketone carbonyl (39), the reaction did afford a dominant diastereomer that was assigned based on the X-ray crystal
structure of the isolated compound 14{44}. Screening the full
compound set for κ opioid, sigma 1, and sigma 2 receptor binding
(Ki values) revealed a number of compounds with modest binding
for these targets. Thus, compound 14{11} emerged as the most
potent Sig-R binding candidate (Ki ¼ 867, 280 nM for sigma 1
and sigma 2, respectively) and compound 14{15} was found to
possess the most potent κ opioid binding (Ki ¼ 407 nM) along
with modest sigma 1 binding (Ki ¼ 1;158 nM). Sixteen of the 44
compounds were also evaluated for 5HT1A binding, with only
compound 14{26} found to possess significant 5HT1A binding activity
(Ki ¼ 431 nM). In addition, four compounds were screened
against the full 43 GPCR assay panel as described previously
for neostenine. The results showed this compound subset to
be free from promiscuous binding, and compound 14{41} was
discovered to possess selective adrenergic binding affinity
(Ki ¼ 1;156, 7,588 nM for Alpha1A and Alpha1B, respectively).
Representative structures of this chemotype and associated
binding activity are shown in Scheme 4 (for complete data on all
compounds, see SI Appendix).
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1楼2011-07-22 08:24:11
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8814402

至尊木虫 (职业作家)

【答案】应助回帖

Although the MCR was not completely diastereoselective, a trend we had previously observed in the reductive amination at the same ketone carbonyl (39), the reaction did afford a dominant diastereomer that was assigned based on the X-ray crystal structure of the isolated compound 14{44}. 尽管我们先前在相同酮羰基化合物的还原性胺化中观察到MCR反应不是完全非对映选择性的，这里的反应确实产生了一个主导性的对映异构体（由分离化合物的X射线衍射晶体结构确定）。Screening the full compound set for κ opioid, sigma 1, and sigma 2 receptor binding (Ki values) revealed a number of compounds with modest binding for these targets. 对全部化合物系列进行的针对k阿片、sigma1和sigma2 受体亲和性的筛选显示了若干对这些受体具有适度亲和性的化合物。
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5楼2011-07-22 09:47:01
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8814402

至尊木虫 (职业作家)

【答案】应助回帖

认领。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。
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2楼2011-07-22 08:40:34
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8814402

至尊木虫 (职业作家)

【答案】应助回帖

★ ★
sltmac(金币+2): 感谢应助~ 2011-07-22 16:06:21
Three potent Sig-R binding compounds—10{20}, 10{22}, and 10{7} (which contains two basic nitrogen atoms)—were evaluated for their GPCR selectivity against 38 targets, and the results were incorporated in Table 1 (see SI Appendix for a heat map– formatted selectivity table). 评估了三种具有强Sig-R亲和性、结构中含有两个碱性氮原子的化合物10{20}, 10{22}和 10{7} 对38种靶标的GPCR选择性，结果总结在表1中。The three compounds displayed >86∶1 selectivities for the limited number of receptors for which binding was observed at all; an impressive result for compounds obtained in such an abbreviated structure-activity optimization exercise.在全部考察了亲和性的受体中，这三种化合物对有限数量的受体显示了>86∶1的选择性；对于通过简单构效优化获得的化合物而言，这是一个给人印象深刻的结果。The N-propyl derivative 10{22}, designed to eliminate binding arising from a pendant aryl-containing side chain, was particularly selective. 被设计以消除由于含芳基侧链而引起的亲和性的 N-丙基衍生物10{20} 表现了突出的选择性。Here, the only non-Sig-R binding was detected against the 5HT1A receptor (Ki ¼ 4;500 nM)     as opposed to Sig-R 1 and Sig-R 2 (Ki values of 12 and 288 nM, respectively), 这里，检测到的唯一的非-Sig-R亲和性是针对与Sig-R 1和2截然相反的5HT1A。
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3楼2011-07-22 09:09:02
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8814402

至尊木虫 (职业作家)

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As part of our efforts toward greater skeletal diversity, additional ring systems were introduced through modifications of the ketone carbonyl on scaffolds constructed by a Diels–Alder/ Schmidt reaction sequence.作为我们增加骨架多样性工作的一部分，通过Diels–Alder/ Schmidt 序列反应对酮羰基加以修饰引入额外的环系统。We applied the isocyanide multicomponent reaction (MCR) methodology developed by Shaabani et al. to transform the ketone carbonyl to the spirocyclic nitrogen heterocycles shown (Scheme 4) (45). 采用由Shaabani 等开发的MCR方法，我们将酮羰基化合物转化为螺环型氮杂环化合物，见示意图4. This protocol smoothly incorporated three elements of diversity in a single operation to afford 44 heterocyclic analogues synthesized from the fragment pool in Scheme 4. 通过恰当的将多样性所需的三个成分整合到一步操作中，实现通过示意图4中所示程序合成44中杂环类似物的目的。This chemotype possesses an intriguing, complex spirocyclic molecular architecture not reported from any natural sources and incorporating three additional basic nitrogen sites. 此化学型具有有趣的尚未见源自天然产物有关报道的复杂螺环分子结构， 含有三个额外的碱性氮点位。
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4楼2011-07-22 09:31:08
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