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10.1021/acs.jmedchem.1c00665 http://scihub22266oqcxt.onion/10.1021/acs.jmedchem.1c00665 34313428!ä!34313428 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       J+Med+Chem 2022 ; 65 (4): 2926-2939 Nephropedia Template TP {{tp|p=34313428|t=2022. 3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV-2 Agents |pdf=|usr=}}{{34313428}} gab.com Text 3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV-2 Agents JO: J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=34313428 #FOAvip The novel coronavirus, SARS-CoV-2, has been identified as the causative agent for the current coronavirus disease (COVID-19) pandemic. 3CL protease (3CL(pro)) plays a pivotal role in the processing of viral polyproteins. We report peptidomimetic compounds with a unique benzothiazolyl ketone as a warhead group, which display potent activity against SARS-CoV-2 3CL(pro). The most potent inhibitor YH-53 can strongly block the SARS-CoV-2 replication. X-ray structural analysis revealed that YH-53 establishes multiple hydrogen bond interactions with backbone amino acids and a covalent bond with the active site of 3CL(pro). Further results from computational and experimental studies, including an in vitro absorption, distribution, metabolism, and excretion profile, in vivo pharmacokinetics, and metabolic analysis of YH-53 suggest that it has a high potential as a lead candidate to compete with COVID-19. Twit Text FOAVip 3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV-2 Agents ????J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=34313428 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=34313428 #FOAvip English Wikipedia <ref>{{Cite pmid|34313428}}</ref> 3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV-2 Agents #MMPMID34313428 Konno S; Kobayashi K; Senda M; Funai Y; Seki Y; Tamai I; Schakel L; Sakata K; Pillaiyar T; Taguchi A; Taniguchi A; Gutschow M; Muller CE; Takeuchi K; Hirohama M; Kawaguchi A; Kojima M; Senda T; Shirasaka Y; Kamitani W; Hayashi Y J Med Chem 2022[Feb]; 65 (4): 2926-2939 PMID34313428show ga The novel coronavirus, SARS-CoV-2, has been identified as the causative agent for the current coronavirus disease (COVID-19) pandemic. 3CL protease (3CL(pro)) plays a pivotal role in the processing of viral polyproteins. We report peptidomimetic compounds with a unique benzothiazolyl ketone as a warhead group, which display potent activity against SARS-CoV-2 3CL(pro). The most potent inhibitor YH-53 can strongly block the SARS-CoV-2 replication. X-ray structural analysis revealed that YH-53 establishes multiple hydrogen bond interactions with backbone amino acids and a covalent bond with the active site of 3CL(pro). Further results from computational and experimental studies, including an in vitro absorption, distribution, metabolism, and excretion profile, in vivo pharmacokinetics, and metabolic analysis of YH-53 suggest that it has a high potential as a lead candidate to compete with COVID-19. |Animals[MESH] |Antiviral Agents/chemical synthesis/chemistry/*pharmacology[MESH] |COVID-19 Drug Treatment[MESH] |COVID-19/metabolism[MESH] |Chlorocebus aethiops[MESH] |Coronavirus 3C Proteases/*antagonists & inhibitors/isolation & purification/metabolism[MESH] |Cysteine Proteinase Inhibitors/chemical synthesis/chemistry/*pharmacology[MESH] |Humans[MESH] |Ketones/chemistry/*pharmacology[MESH] |Male[MESH] |Microbial Sensitivity Tests[MESH] |Microsomes, Liver/chemistry/metabolism[MESH] |Models, Molecular[MESH] |Molecular Conformation[MESH] |Peptidomimetics/chemical synthesis/chemistry/*pharmacology[MESH] |Rats[MESH] |Rats, Wistar[MESH] |SARS-CoV-2/*drug effects/enzymology[MESH]3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as An(epmc).pdf DeepDyve Pubget Overpricing