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在纯溶剂和二元介质中探测偶氮键前药的溶剂-溶质相互作用:实验与计算的综合研究。

Probing the Solute-Solvent Interaction of an Azo-Bonded Prodrug in Neat and Binary Media: Combined Experimental and Computational Study.

机构信息

Department of Chemistry & Earth Sciences, College of Arts & Science, Qatar University, Doha, State of Qatar.

出版信息

Sci Rep. 2019 Feb 28;9(1):3023. doi: 10.1038/s41598-019-39028-1.

Abstract

Preferential solvation has significant importance in interpreting the molecular physicochemical properties of wide spectrum of materials in solution. In this work, the solute-solvent interaction of pro-drug Sulfasalazine (SSZ) in neat and binary media was investigated experimentally and computationally. The solute-solvent interactions of interest were spectrophotometrically probed and computationally investigated for providing insights concerning the molecular aspects of SSZ:media interaction. Experimentally, the obtained results in 1,4-dioxane:water binary mixture demonstrated a dramatic non-linear changes in the spectral behavior of SSZ indicative of the dependency of its molecular behaviors on the compositions of the molecular microenvironment in the essence of solute-solvent interaction. Computationally, geometry optimization and simulation of the absorption spectra of SSZ in media of interest were performed employing DFT and TD-DFT methods, respectively, where the solvent effects on the absorption were examined implicitly using IEFPCM method. Obtained results revealed a nonpolar nature of the molecular orbitals that are directly involved in the SSZ:medium interaction. As in good correspondence with the experimental results, these simulations demonstrated that these orbitals are of non-polar nature and hence minimally affected by polarity of the media and in turn favoring the non-polar molecular environments. On the other hand, the molecular origin of SSZ:media interaction was demonstrated explicitly through complexation of SSZ with water molecules revealing a cooperative hydrogen bonding stabilization with an average length of 1.90 Å. The findings of this work demonstrate the significance of the preferential solvation and composition of the molecular microenvironment on the physicochemical properties of molecules of pharmaceutical importance.

摘要

优先溶剂化在解释广泛范围内物质在溶液中的分子物理化学性质方面具有重要意义。在这项工作中,实验和计算研究了前药柳氮磺胺吡啶(SSZ)在纯相和二元介质中的溶质-溶剂相互作用。通过分光光度法探测溶质-溶剂相互作用,并进行计算研究,以提供有关 SSZ 的分子方面的见解:介质相互作用。实验上,在 1,4-二恶烷:水二元混合物中获得的结果表明 SSZ 的光谱行为发生了剧烈的非线性变化,表明其分子行为依赖于分子微环境的组成,实质上是溶质-溶剂相互作用的结果。计算上,采用 DFT 和 TD-DFT 方法分别对 SSZ 在感兴趣的介质中的吸收光谱进行了几何优化和模拟,其中使用 IEFPCM 方法隐式地检查了溶剂对吸收的影响。得到的结果表明,直接参与 SSZ:介质相互作用的分子轨道具有非极性性质。与实验结果非常吻合,这些模拟表明这些轨道具有非极性性质,因此受介质极性的影响很小,从而有利于非极性分子环境。另一方面,通过 SSZ 与水分子的络合,明确地证明了 SSZ:介质相互作用的分子起源,揭示了平均长度为 1.90 Å 的协同氢键稳定作用。这项工作的发现表明,优先溶剂化和分子微环境的组成对具有药物重要性的分子的物理化学性质具有重要意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4d9e/6395765/7de803cfffae/41598_2019_39028_Fig1_HTML.jpg

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