Department of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre utca 9, 1092 Budapest, Hungary.
Department of Organic Chemistry, Semmelweis University, Hőgyes Endre utca 7, 1092 Budapest, Hungary.
Int J Mol Sci. 2023 Dec 28;25(1):412. doi: 10.3390/ijms25010412.
The presence of a chiral or chirally perturbed chromophore in the molecule under investigation is a fundamental requirement for the appearance of a circular dichroism (CD) spectrum. For native and for most of the substituted cyclodextrins, this condition is not applicable, because although chiral, cyclodextrins lack a chromophore group and therefore have no characteristic CD spectra over 220 nm. The reason this method can be used is that if the guest molecule has a chromophore group and this is in the right proximity to the cyclodextrin, it becomes chirally perturbed. As a result, the complex will now provide a CD signal, and this phenomenon is called induced circular dichroism (ICD). The appearance of the ICD spectrum is clear evidence of the formation of the complex, and the spectral sign and intensity is a good predictor of the structure of the complex. By varying the concentration of cyclodextrin, the ICD signal changes, resulting in a saturation curve, and from these data, the stability constant can be calculated for a 1:1 complex. This article compares ICD and NMR spectroscopic and molecular modeling results of cyclodextrin complexes of four model compounds: nimesulide, fenbufen, fenoprofen, and bifonazole. The results obtained by the different methods show good agreement, and the structures estimated from the ICD spectra are supported by NMR data and molecular modeling.
在被研究的分子中存在手性或手性扰动的发色团是出现圆二色性(CD)光谱的基本要求。对于天然和大多数取代的环糊精,这种情况并不适用,因为尽管手性,环糊精缺乏发色团,因此在 220nm 以上没有特征 CD 光谱。之所以可以使用这种方法,是因为如果客体分子具有发色团,并且该发色团与环糊精的距离合适,则它会受到手性扰动。结果,该复合物现在将提供 CD 信号,这种现象称为诱导圆二色性(ICD)。ICD 光谱的出现清楚地证明了复合物的形成,并且光谱的符号和强度是复合物结构的良好预测指标。通过改变环糊精的浓度,ICD 信号发生变化,导致饱和曲线,并且可以根据这些数据计算出 1:1 复合物的稳定常数。本文比较了四种模型化合物(尼美舒利、布洛芬、芬布芬和比佛拉唑)的环糊精复合物的 ICD 和 NMR 光谱学和分子建模结果。不同方法获得的结果具有良好的一致性,并且从 ICD 光谱估计的结构得到 NMR 数据和分子建模的支持。