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New insights in the mechanism of the SARS-CoV-2 M(pro) inhibition by benzisoselenazolones and diselenides.
Sancineto L, Mangiavacchi F, Dabrowska A, Pacuła-Miszewska AJ, Obieziurska-Fabisiak M, Scimmi C, Ceccucci V, Kong J, Zhao Y, Ciancaleoni G, Nascimento V, Rizzuti B, Bortoli M, Orian L, Kula-Pacurar A, Yang H, Ścianowski J, Lei Y, Pyrc K, Santi C. Sancineto L, et al. Sci Rep. 2024 Oct 21;14(1):24751. doi: 10.1038/s41598-024-75519-6. Sci Rep. 2024. PMID: 39433805 Free PMC article.
Although global vaccination campaigns alleviated the SARS-CoV-2 pandemic in terms of morbidity and mortality, the ability of the virus to originate mutants may reduce the efficacy of vaccines, posing a serious risk of a renewed pandemic. ...The overall result …
Although global vaccination campaigns alleviated the SARS-CoV-2 pandemic in terms of morbidity and mortality, the abili …
Asymmetric imidazole-4,5-dicarboxamide derivatives as SARS-CoV-2 main protease inhibitors: design, synthesis and biological evaluation.
Huynh PNH, Khamplong P, Phan MH, Nguyen TP, Vu PNL, Tang QV, Chamsodsai P, Seetaha S, Tuong TL, Vu TY, Vo DD, Choowongkomon K, Vo CT. Huynh PNH, et al. RSC Med Chem. 2024 Sep 3;15(11):3880-8. doi: 10.1039/d4md00414k. Online ahead of print. RSC Med Chem. 2024. PMID: 39345712 Free article.
The SARS-CoV-2 main protease, a vital enzyme for virus replication, is a potential target for developing drugs in COVID-19 treatment. Until now, three SARS-CoV-2 main protease inhibitors have been approved for COVID- …
The SARS-CoV-2 main protease, a vital enzyme for virus replication, is a potential target for developing drugs in CO …
SARS-CoV-2 replication and drug discovery.
Nazir F, John Kombe Kombe A, Khalid Z, Bibi S, Zhang H, Wu S, Jin T. Nazir F, et al. Mol Cell Probes. 2024 Oct;77:101973. doi: 10.1016/j.mcp.2024.101973. Epub 2024 Jul 24. Mol Cell Probes. 2024. PMID: 39025272 Free article. Review.
The coronavirus disease 2019 (COVID-19) caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has killed millions of people and continues to wreak havoc across the globe. ...Indeed, based on the molecular similarity approach …
The coronavirus disease 2019 (COVID-19) caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV- …
Machine learning-based QSAR and LB-PaCS-MD guided design of SARS-CoV-2 main protease inhibitors.
Toopradab B, Xie W, Duan L, Hengphasatporn K, Harada R, Sinsulpsiri S, Shigeta Y, Shi L, Maitarad P, Rungrotmongkol T. Toopradab B, et al. Bioorg Med Chem Lett. 2024 Sep 15;110:129852. doi: 10.1016/j.bmcl.2024.129852. Epub 2024 Jun 24. Bioorg Med Chem Lett. 2024. PMID: 38925524
The global outbreak of the COVID-19 pandemic caused by the SARS-CoV-2 virus had led to profound respiratory health implications. This study focused on designing organoselenium-based inhibitors targeting the SARS-CoV-2 main p …
The global outbreak of the COVID-19 pandemic caused by the SARS-CoV-2 virus had led to profound respirato …
Development of a Biosafety Level 1 Cellular Assay for Identifying Small-Molecule Antivirals Targeting the Main Protease of SARS-CoV-2: Evaluation of Cellular Activity of GC376, Boceprevir, Carmofur, Ebselen, and Selenoneine.
Fukumoto Y, Suzuki N, Hara R, Tanaka YK, Ogra Y. Fukumoto Y, et al. Int J Mol Sci. 2024 May 25;25(11):5767. doi: 10.3390/ijms25115767. Int J Mol Sci. 2024. PMID: 38891954 Free PMC article.
While research has identified several inhibitors of the main protease (Mpro) of SARS-CoV-2, a significant portion of these compounds exhibit reduced activity in the presence of reducing agents, raising concerns about their effectiveness in vivo. ...Using this …
While research has identified several inhibitors of the main protease (Mpro) of SARS-CoV-2, a significant portion of th …
Reaction Pattern and Mechanistic Aspects of Iodine and Iodine-Based Reagents in Selenylation of Aliphatic, Aromatic, and (Hetero)Cyclic Systems.
Kumar P, Bhalla A. Kumar P, et al. Top Curr Chem (Cham). 2024 Apr 8;382(2):12. doi: 10.1007/s41061-024-00459-8. Top Curr Chem (Cham). 2024. PMID: 38589598 Review.
Organoselenium compounds have been the subject of extensive research since the discovery of the biologically active compound ebselen. Ebselen has recently been found to show activity against the main protease of the virus responsible for COVID-19. ...
Organoselenium compounds have been the subject of extensive research since the discovery of the biologically active compound ebselen. …
Improved fluorescence-based assay for rapid screening and evaluation of SARS-CoV-2 main protease inhibitors.
Zhang R, Yan H, Zhou J, Yan G, Liu X, Shang C, Chen Y. Zhang R, et al. J Med Virol. 2024 Mar;96(3):e29498. doi: 10.1002/jmv.29498. J Med Virol. 2024. PMID: 38436148
The outbreak of coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a global threat to human health. In parallel with vaccines, efficacious antivirals are urgently needed. …
The outbreak of coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2 ( …
Repurposing ebselen as an inhalable dry powder to treat respiratory tract infections.
Saha T, Lyons N, Yue Yung DB, Quiñones-Mateu ME, Pletzer D, Das SC. Saha T, et al. Eur J Pharm Biopharm. 2024 Feb;195:114170. doi: 10.1016/j.ejpb.2023.12.010. Epub 2023 Dec 19. Eur J Pharm Biopharm. 2024. PMID: 38128743 Free article.
While antimicrobial resistance could be overcome by developing new antimicrobial agents, the use of a safe repurposed agent having potent antimicrobial activity against various RTIs can be an efficient and cost-effective alternative to overcome the long and complex process of dev …
While antimicrobial resistance could be overcome by developing new antimicrobial agents, the use of a safe repurposed agent having potent an …
Inhibitory effects against SARSCoV-2 main protease (Mpro) of biflavonoids and benzophenones from the fruit of Platonia insignis.
Moreira Costa MA, de Sousa NF, Mansur Pontes CL, Scotti MT, de Assis FF, Braga AL, Sandjo LP. Moreira Costa MA, et al. Fitoterapia. 2024 Mar;173:105784. doi: 10.1016/j.fitote.2023.105784. Epub 2023 Dec 19. Fitoterapia. 2024. PMID: 38128621
The SARS-CoV-2 mutation and the limitation of the approved drug against COVID-19 are still a challenge in many country healthcare systems and need to be affronted despite the set of vaccines to prevent this viral infection. To contribute to the …
The SARS-CoV-2 mutation and the limitation of the approved drug against COVID-19 are still a challenge in …
Identification of Ebselen derivatives as novel SARS-CoV-2 main protease inhibitors: Design, synthesis, biological evaluation, and structure-activity relationships exploration.
Zhang H, Li J, Toth K, Tollefson AE, Jing L, Gao S, Liu X, Zhan P. Zhang H, et al. Bioorg Med Chem. 2023 Dec 15;96:117531. doi: 10.1016/j.bmc.2023.117531. Epub 2023 Nov 11. Bioorg Med Chem. 2023. PMID: 37972434
The main protease (M(pro)) represents one of the most effective and attractive targets for designing anti-SARS-CoV-2 drugs. In this study, we designed and synthesized a novel series of Ebselen derivatives by incorporating privileged fragments from diff …
The main protease (M(pro)) represents one of the most effective and attractive targets for designing anti-SARS-CoV-2 dr …
72 results