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2-甲氧基-4,6-二苯基烟腈的结构、功能与ADMET综合分析:X射线衍射、分子对接、动力学模拟及先进计算见解的融合

Integrated Structural, Functional, and ADMET Analysis of 2-Methoxy-4,6-diphenylnicotinonitrile: The Convergence of X-ray Diffraction, Molecular Docking, Dynamic Simulations, and Advanced Computational Insights.

作者信息

Bakheit Ahmed H, Alkahtani Hamad M

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.

出版信息

Molecules. 2023 Sep 28;28(19):6859. doi: 10.3390/molecules28196859.

Abstract

This study systematically investigates the molecular structure and electronic properties of 2-methoxy-4,6-diphenylnicotinonitrile, employing X-ray diffraction (XRD) and sophisticated computational methodologies. XRD findings validate the compound's orthorhombic crystallization in the P21212 space group, composed of a pyridine core flanked by two phenyl rings. Utilizing the three-dimensional Hirshfeld surface, the research decodes the molecule's spatial attributes, further supported by exhaustive statistical assessments. Key interactions, such as π-π stacking and H⋯X contacts, are spotlighted, underscoring their role in the crystal's inherent stability and characteristics. Energy framework computations and density functional theory (DFT) analyses elucidate the prevailing forces in the crystal and reveal geometric optimization facets and molecular reactivity descriptors. Emphasis is given to the exploration of frontier molecular orbitals (FMOs), aromaticity, and π-π stacking capacities. The research culminates in distinguishing electron density distributions, aromatic nuances, and potential reactivity hotspots, providing a holistic view of the compound's structural and electronic landscape. Concurrently, molecular docking investigates its interaction with the lipoprotein-associated phospholipase A2 protein. Notably, the compound showcases significant interactions with the protein's active site. Molecular dynamics simulations reveal the compound's influence on protein stability and flexibility. Although the molecule exhibits strong inhibitory potential against Lp-PLA2, its drug development prospects face challenges related to solubility and interactions with drug transport proteins.

摘要

本研究采用X射线衍射(XRD)和先进的计算方法,系统地研究了2-甲氧基-4,6-二苯基烟腈的分子结构和电子性质。XRD结果证实该化合物在P21212空间群中呈正交晶型,由一个吡啶核心和两个苯环组成。利用三维Hirshfeld表面,该研究解析了分子的空间属性,并通过详尽的统计评估进一步得到支持。突出了关键相互作用,如π-π堆积和H⋯X接触,强调了它们在晶体固有稳定性和特性中的作用。能量框架计算和密度泛函理论(DFT)分析阐明了晶体中的主要作用力,并揭示了几何优化方面和分子反应性描述符。重点探索了前沿分子轨道(FMO)、芳香性和π-π堆积能力。该研究最终区分了电子密度分布、芳香细微差别和潜在的反应性热点,提供了该化合物结构和电子景观的整体视图。同时,分子对接研究了其与脂蛋白相关磷脂酶A2蛋白的相互作用。值得注意的是,该化合物与蛋白质的活性位点表现出显著的相互作用。分子动力学模拟揭示了该化合物对蛋白质稳定性和灵活性的影响。尽管该分子对Lp-PLA2具有很强的抑制潜力,但其药物开发前景面临与溶解度以及与药物转运蛋白相互作用相关的挑战。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7a62/10574294/69fc113a6764/molecules-28-06859-g001.jpg

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