基于双硫代氨基脲的新型双噻唑类抗柯萨奇病毒药物的合成、表征、分子对接、药代动力学和分子动力学。

IF 3.8 2区 综合性期刊 Q1 MULTIDISCIPLINARY SCIENCES
Thoraya A Farghaly, Eman M H Abbas, Heba S Abd-Elghaffar, Mohamed A Elsayed, Dina H Elnaggar, Ahmed F El-Sayed, Dina N Abd-Elshafy, Salwa F Mohamed
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引用次数: 0

摘要

众所周知,大多数病毒感染开始时都是皮肤糜烂,大多数情况下会自行痊愈。与其他感染性疾病一样,预后取决于免疫监视状态。因此,免疫抑制者的危险性更大。但近来人们越来越清楚地认识到,曾经被认为是良性疾病的糜烂,即使在免疫功能正常的患者中,也可能真正导致问题甚至死亡。因此,在这篇文章中,我们的目标是找出可能的潜在抗病毒候选物。我们通过双硫代氨基甲酮衍生物 3 与肼酰氯和卤代酮类化合物的反应合成了一系列双噻唑衍生物,试图研究它们潜在的抗病毒特性以及与柯萨奇病毒 B 主要蛋白酶的相互作用。研究发现,最有效的衍生物双噻唑衍生物 7a 对柯萨奇病毒 B(Cox B)具有最强的抗病毒活性。对其作用模式的进一步研究表明,化合物 7a 具有抑制病毒吸附和复制的双重活性。利用分子对接技术评估了许多化合物对柯萨奇病毒腺病毒靶标的功效。研究结果表明,化合物 7a、7c、11b 和 11c 具有很高的结合能,能有效地与柯萨奇病毒腺病毒受体 (CAR)、3C 蛋白酶和 RNA 依赖性 RNA 聚合酶 (RdRp) 等柯萨奇病毒 B 病毒重要蛋白的活性位点结合。这些相互作用涉及多种化学键类型,表明这些物质在抑制酶活性的同时,还能在病毒复制和吸附方面发挥巨大的抗病毒作用。此外,对这些化合物进行的 ADMET 计算研究表明,它们符合利宾斯基标准,这意味着它们具有积极的理化特性。此外,MD 模拟还证明了 7a 和 11b 与柯萨奇病毒腺病毒受体 (CAR)、3C 蛋白酶和 RNA 依赖性 RNA 聚合酶 (RdRp) 的稳定复合物,其 RMSD(0.1-0.30、0.20-0.30 和 0.20-0.35 nm)、RMSF(0.1-0.5 nm)和 SASA(80-105、140-150 和 220-235)。这些结果进一步增强了这些化合物在当前抗病毒药物开发工作中的潜力。这些研究结果强调了这些化合物作为柯萨奇病毒腺病毒抗病毒疗法候选药物的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, characterization, molecular docking, pharmacokinetics, and molecular dynamics of new bis-thiazoles based on bis-thiosemicarbazone as anti-coxsackievirus.

It was known that the majority of viral infections start off as cutaneous eruptions, which heal on their own in most cases. The prognosis is dependent on the state of immunologic surveillance, just like in other infectious disorders. Therefore, those who are immunosuppressed are more in danger. But recently it's becoming increasingly clear that eruptions that were once thought to be benign diseases can really cause problems and even death, even in immunocompetent patients. Hence, in this article, our goal was to identify possible potential antiviral candidates. We have synthesized a series of bis-thiazole derivatives via the reaction of bis-thiosemicarbazone derivative 3 with hydrazonoyl chlorides and haloketones in an effort to examine their potential antiviral properties and interactions with the main protease of Coxsackievirus B. Spectroscopic methods and elemental analysis were used to corroborate the structures of the novel bis-thiazole derivatives. The most potent derivative, bis-thiazole derivative 7a, was found to have the strongest antiviral activity against Coxsackievirus B (Cox B). Further investigation into its mode of action indicated that compound 7a has a dual activity that inhibits viral adsorption and replication. The efficacy of many compounds against Coxsackievirus adenovirus targets was assessed using molecular docking. The findings revealed that compounds 7a, 7c, 11b and 11c have high binding energies, efficiently engaging the active sites of essential Cox B virus proteins such as the Coxsackievirus adenovirus receptor (CAR), 3C-protease, and RNA-dependent RNA polymerase (RdRp). These interactions involved a variety of chemical bonding types, indicating that these substances can inhibit enzyme activity while also exhibiting substantial antiviral effects involving viral replication and adsorption. Furthermore, the computational ADMET study of these compounds indicated conformance to Lipinski's criteria, implying positive physicochemical properties. Furthermore, MD simulations demonstrated stable complexes of 7a and 11b with Coxsackievirus adenovirus receptor (CAR), 3C-protease, and RNA dependent RNA polymerase (RdRp) with RMSD (0.1-0.30, 0.20-0.30, and 0.20-0.35 nm), RMSF (0.1-0.5 nm), and SASA (80-105, 140-150, and 220-235). These outcomes further reinforce the potential of these compounds in current antiviral drug development endeavors. The collective findings underscore the potential of these compounds as candidates for antiviral therapies against Coxsackievirus adenovirus.

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来源期刊
Scientific Reports
Scientific Reports Natural Science Disciplines-
CiteScore
7.50
自引率
4.30%
发文量
19567
审稿时长
3.9 months
期刊介绍: We publish original research from all areas of the natural sciences, psychology, medicine and engineering. You can learn more about what we publish by browsing our specific scientific subject areas below or explore Scientific Reports by browsing all articles and collections. Scientific Reports has a 2-year impact factor: 4.380 (2021), and is the 6th most-cited journal in the world, with more than 540,000 citations in 2020 (Clarivate Analytics, 2021). •Engineering Engineering covers all aspects of engineering, technology, and applied science. It plays a crucial role in the development of technologies to address some of the world''s biggest challenges, helping to save lives and improve the way we live. •Physical sciences Physical sciences are those academic disciplines that aim to uncover the underlying laws of nature — often written in the language of mathematics. It is a collective term for areas of study including astronomy, chemistry, materials science and physics. •Earth and environmental sciences Earth and environmental sciences cover all aspects of Earth and planetary science and broadly encompass solid Earth processes, surface and atmospheric dynamics, Earth system history, climate and climate change, marine and freshwater systems, and ecology. It also considers the interactions between humans and these systems. •Biological sciences Biological sciences encompass all the divisions of natural sciences examining various aspects of vital processes. The concept includes anatomy, physiology, cell biology, biochemistry and biophysics, and covers all organisms from microorganisms, animals to plants. •Health sciences The health sciences study health, disease and healthcare. This field of study aims to develop knowledge, interventions and technology for use in healthcare to improve the treatment of patients.
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