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首页> 外文期刊>Chemistry: A European journal >An extraction-based assay for neutral anionophores: the measurement of high binding constants to steroidal receptors in a nonpolar solvent
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An extraction-based assay for neutral anionophores: the measurement of high binding constants to steroidal receptors in a nonpolar solvent

机译：基于提取的中性阴离子载体测定：在非极性溶剂中对甾体受体的高结合常数的测量

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摘要

The extraction-based protocol for measuring binding constants, developed by Cram and co-workers, has been extended for use with anionic substrates. The method is especially useful for high-affinity receptors, allowing very high binding constants to be measured in nonpolar solvents. Distribution constants K_d bentween chloroform and water have been obtained for tetraethylammonium chloride and bromide, thus calibrating the method for these two substrates. Application to steroidal podands 5-9 has confirmed the ability of electron-withdarwing groups to enhance hydrogen- bond donor capabilities. Binding constants of approx= 3 X 10~7 M~(-1) have been measured for the most powerful receptor 7. An X-ray crystal structure of 15, the methyl ester analogue or 7, reveals a well-defined binding site preorganised for anion recognition.
机译：由Cram和同事开发的基于萃取的用于测量结合常数的方案已扩展为可与阴离子底物一起使用。该方法对高亲和力受体特别有用，可以在非极性溶剂中测量非常高的结合常数。对于四乙基氯化铵和溴化物，已经获得了氯仿和水之间的分布常数K_d，因此对这两种底物的方法进行了校准。应用于类固醇podand 5-9已经证实了具有电子负性基团增强氢键供体能力的能力。对于最强大的受体7，已测得结合常数约为3 X 10〜7 M〜（-1）。X射线晶体结构15，甲酯类似物或7揭示了预先定义好的结合位点用于阴离子识别。

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