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Summary and Final Comments. In this study, we have identified three sets of biaoctive compounds based on the tricyclic core of the Stemona alkaloid skeleton shown in Fig. 6. These compounds vary in their degrees of added structural complexity from a simple amide reduction (6{10}) to a greater than twofold increase of the molecular weight via an isocyanide MCR (14{26}). Each of these compounds has provided potent binding compounds that may be viewed as lead structures for further development. Moreover, we identified a particular chemical feature consistent with activity (a basic nitrogen atom), which suggested a scaffold-hopping maneuver that resulted in unique compounds with exquisite potency and selectivity against the Sig-Rs. |
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8814402
至尊木虫 (职业作家)
- 翻译EPI: 509
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- 专业: 药物学其他科学问题
2楼2011-07-20 10:07:44
8814402
至尊木虫 (职业作家)
- 翻译EPI: 509
- 应助: 18 (小学生)
- 贵宾: 0.381
- 金币: 12916.1
- 散金: 47
- 红花: 16
- 帖子: 4183
- 在线: 357.8小时
- 虫号: 1184404
- 注册: 2011-01-06
- 专业: 药物学其他科学问题
【答案】应助回帖
★
liugy2009(金币+40, 翻译EPI+1): O(∩_∩)O~~~谢谢帮忙 2011-07-20 19:19:34
Mally89(金币+1): 感谢应助！~ 2011-07-23 22:02:26
liugy2009(金币+40, 翻译EPI+1): O(∩_∩)O~~~谢谢帮忙 2011-07-20 19:19:34
Mally89(金币+1): 感谢应助！~ 2011-07-23 22:02:26
| Summary and Final Comments.总结和最后评论 In this study, we have identified three sets of biaoctive compounds based on the tricyclic core of the Stemona alkaloid skeleton shown in Fig. 6. 本研究中，我们鉴定了基于斯替宁碱骨架三环核心的三个系列的活性化合物，见图6.These compounds vary in their degrees of added structural complexity from a simple amide reduction (6{10}) to a greater than twofold increase of the molecular weight via an isocyanide MCR (14{26}).这些化合物在增加的结构复杂性上各不相同。 Each of these compounds has provided potent binding compounds that may be viewed as lead structures for further development. 每种系列化合物都可选出可视作进一步开发的先导化合物的高亲和性化合物。Moreover, we identified a particular chemical feature consistent with activity (a basic nitrogen atom), which suggested a scaffold-hopping maneuver that resulted in unique compounds with exquisite potency and selectivity against the Sig-Rs.而且，我们还鉴定了与活性一致的一种特殊的化学特征---碱性氮原子，这提示支架变换策略可得到对Sig-R具有强烈活性和灵敏选择性的独特化合物。 |
3楼2011-07-20 11:24:06