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 0.20-0.35Â nm), RMSF (0.1-0.5Â 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.
Synthesis, characterization, molecular docking, pharmacokinetics, and molecular dynamics of new bis-thiazoles based on bis-thiosemicarbazone as anti-coxsackievirus.
阅读:6
作者:Farghaly Thoraya A, Abbas Eman M H, Abd-Elghaffar Heba S, Elsayed Mohamed A, Elnaggar Dina H, El-Sayed Ahmed F, Abd-Elshafy Dina N, Mohamed Salwa F
| 期刊: | Scientific Reports | 影响因子: | 3.900 |
| 时间: | 2024 | 起止号: | 2024 Nov 26; 14(1):29378 |
| doi: | 10.1038/s41598-024-80753-z | ||
特别声明
1、本文转载旨在传播信息,不代表本网站观点,亦不对其内容的真实性承担责任。
2、其他媒体、网站或个人若从本网站转载使用,必须保留本网站注明的“来源”,并自行承担包括版权在内的相关法律责任。
3、如作者不希望本文被转载,或需洽谈转载稿费等事宜,请及时与本网站联系。
4、此外,如需投稿,也可通过邮箱info@biocloudy.com与我们取得联系。
