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何超

金虫 (正式写手)


[交流] 文献理解

为了作业,在精读一篇Bioorganic&Medicinal  Chemistry  Letters上的英文文献,对其中一点关于实验结果的内容理解有问题,觉得文字叙述内容与表格所给的结果不一致,盼各位指点......
内容如下:
Modification of the amino substituent gave the isomeric tetramethyl derivative 17 and the 4,7-dihydroindanyl indacaterol derivative 29 which had comparable decreases in affinity and selectivity when compared to 1. The 5-n-butylindanyl analogue 16, as a diasteroisomeric mixture epimeric at the 2-indanyl position, exhibited a similar binding profile to 1, suggesting the potential for a similar overall profile. However, the additional stereochemical complexity in 16 reduced the attractiveness of this analogue for further follow up studies. Introduction of the a-methyl group into the amino substituent gave the analogue 25 which led to the anticipated increase in b2adrenoceptor affinity, of greater than 10-fold relative to 1.However, this increase in affinity was also accompanied by an even greater relative increase in b1-adrenoceptor affinity and an overall reduction in binding selectivity.
表如下:(附件里,弄不上来)
希望各位不吝各抒己见,指导指导我这个马上要交作业的人......

HW5~KR45$B1]T(5S6J@{`X4.jpg
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何超

金虫 (正式写手)


我的理解,化合物17、29,文字叙述说对b2肾上腺素受体的亲和力和选择都下降,而表的内容显示应该是都升高的
还有关于化合物25的叙述说对b2肾上腺素受体的亲和力增加,表里内容是降低的
你们可能会说,是我对那个K的意义理解错了,我觉得应该是结合的速率与分解的速率之比,而且根据这一理解能与前面关于其他化合物的叙述相符
不知道是怎么回事,盼指教......
2楼2012-10-23 19:43:46
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何超

金虫 (正式写手)


是因为看到一大段的英文而没人回么?
请就看这3句:
化合物17、29的  Modification of the amino substituent gave the isomeric tetramethyl derivative 17 and the 4,7-dihydroindanyl indacaterol derivative 29 which had comparable decreases in affinity and selectivity when compared to 1.
化合物16的    Introduction of the a-methyl group into the amino substituent gave the analogue 25 which led to the anticipated increase in b2adrenoceptor affinity, of greater than 10-fold relative to 1.However, this increase in affinity was also accompanied by an even greater relative increase in b1-adrenoceptor affinity and an overall reduction in binding selectivity.
谢谢!!!
3楼2012-10-24 08:44:25
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何超

金虫 (正式写手)


引用回帖:
4楼: Originally posted by 郑克宁 at 2012-10-24 09:01:23

感谢支持!!!
不吝赐教!!!
6楼2012-10-24 16:26:33
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何超

金虫 (正式写手)


引用回帖:
5楼: Originally posted by jiangsishui at 2012-10-24 09:07:50

感谢回复,不吝赐教!!!
7楼2012-10-24 16:27:10
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简单回复
郑克宁4楼
2012-10-24 09:01  
2012-10-24 09:07  
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