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10.1016/j.bioorg.2021.104889 http://scihub22266oqcxt.onion/10.1016/j.bioorg.2021.104889 33915460!8026246!33915460     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Bioorg+Chem 2021 ; 112 (ä): 104889 Nephropedia Template TP {{tp|p=33915460|t=2021. Ebsulfur and Ebselen as highly potent scaffolds for the development of potential SARS-CoV-2 antivirals |pdf=|usr=}}{{33915460}} gab.com Text Ebsulfur and Ebselen as highly potent scaffolds for the development of potential SARS-CoV-2 antivirals JO: Bioorg Chem http://www.kidney.de/pget.php?&tw=1&pmid=33915460 #FOAvip The emerging COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has raised a global catastrophe. To date, there is no specific antiviral drug available to combat this virus, except the vaccine. In this study, the main protease (M(pro)) required for SARS-CoV-2 viral replication was expressed and purified. Thirty-six compounds were tested as inhibitors of SARS-CoV-2 M(pro) by fluorescence resonance energy transfer (FRET) technique. The half-maximal inhibitory concentration (IC(50)) values of Ebselen and Ebsulfur analogs were obtained to be in the range of 0.074-0.91 muM. Notably, the molecules containing furane substituent displayed higher inhibition against M(pro), followed by Ebselen 1i (IC(50) = 0.074 muM) and Ebsulfur 2k (IC(50) = 0.11 muM). The action mechanism of 1i and 2k were characterized by enzyme kinetics, pre-incubation and jump dilution assays, as well as fluorescent labeling experiments, which suggested that both compounds covalently and irreversibly bind to M(pro), while molecular docking suggested that 2k formed an SS bond with the Cys145 at the enzymatic active site. This study provides two very potent scaffolds Ebsulfur and Ebselen for the development of covalent inhibitors of M(pro) to combat COVID-19. Twit Text FOAVip Ebsulfur and Ebselen as highly potent scaffolds for the development of potential SARS-CoV-2 antivirals ????Bioorg Chem http://www.kidney.de/pget.php?&tw=1&pmid=33915460 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33915460 #FOAvip English Wikipedia <ref>{{Cite pmid|33915460}}</ref> Ebsulfur and Ebselen as highly potent scaffolds for the development of potential SARS-CoV-2 antivirals #MMPMID33915460 Sun LY; Chen C; Su J; Li JQ; Jiang Z; Gao H; Chigan JZ; Ding HH; Zhai L; Yang KW Bioorg Chem 2021[Jul]; 112 (ä): 104889 PMID33915460show ga The emerging COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has raised a global catastrophe. To date, there is no specific antiviral drug available to combat this virus, except the vaccine. In this study, the main protease (M(pro)) required for SARS-CoV-2 viral replication was expressed and purified. Thirty-six compounds were tested as inhibitors of SARS-CoV-2 M(pro) by fluorescence resonance energy transfer (FRET) technique. The half-maximal inhibitory concentration (IC(50)) values of Ebselen and Ebsulfur analogs were obtained to be in the range of 0.074-0.91 muM. Notably, the molecules containing furane substituent displayed higher inhibition against M(pro), followed by Ebselen 1i (IC(50) = 0.074 muM) and Ebsulfur 2k (IC(50) = 0.11 muM). The action mechanism of 1i and 2k were characterized by enzyme kinetics, pre-incubation and jump dilution assays, as well as fluorescent labeling experiments, which suggested that both compounds covalently and irreversibly bind to M(pro), while molecular docking suggested that 2k formed an SS bond with the Cys145 at the enzymatic active site. This study provides two very potent scaffolds Ebsulfur and Ebselen for the development of covalent inhibitors of M(pro) to combat COVID-19. |Antiviral Agents/chemistry/*metabolism/therapeutic use[MESH] |Azoles/chemistry/*metabolism/therapeutic use[MESH] |Binding Sites[MESH] |COVID-19 Drug Treatment[MESH] |COVID-19/pathology/virology[MESH] |Catalytic Domain[MESH] |Fluorescence Resonance Energy Transfer[MESH] |Humans[MESH] |Inhibitory Concentration 50[MESH] |Isoindoles[MESH] |Kinetics[MESH] |Molecular Docking Simulation[MESH] |Organoselenium Compounds/chemistry/*metabolism/therapeutic use[MESH] |SARS-CoV-2/isolation & purification/*metabolism[MESH] |Structure-Activity Relationship[MESH] |Sulfur Compounds/chemistry/*metabolism/therapeutic use[MESH]Ebsulfur and Ebselen as highly potent scaffolds for the development of(epmc).pdf DeepDyve Pubget Overpricing