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10.1016/j.bmcl.2021.127885

http://scihub22266oqcxt.onion/10.1016/j.bmcl.2021.127885
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33662537!7920804!33662537
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suck abstract from ncbi


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pmid33662537      Bioorg+Med+Chem+Lett 2021 ; 39 (ä): 127885
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  • Design, synthesis and biological evaluation of 2-aminoquinazolin-4(3H)-one derivatives as potential SARS-CoV-2 and MERS-CoV treatments #MMPMID33662537
  • Lee JY; Shin YS; Jeon S; Lee SI; Noh S; Cho JE; Jang MS; Kim S; Song JH; Kim HR; Park CM
  • Bioorg Med Chem Lett 2021[May]; 39 (ä): 127885 PMID33662537show ga
  • Despite the rising threat of fatal coronaviruses, there are no general proven effective antivirals to treat them. 2-Aminoquinazolin-4(3H)-one derivatives were newly designed, synthesized, and investigated to show the inhibitory effects on SARS-CoV-2 and MERS-CoV. Among the synthesized derivatives, 7-chloro-2-((3,5-dichlorophenyl)amino)quinazolin-4(3H)-one (9g) and 2-((3,5-dichlorophenyl)amino)-5-hydroxyquinazolin-4 (3H)-one (11e) showed the most potent anti-SARS-CoV-2 activities (IC(50) < 0.25 muM) and anti-MERS-CoV activities (IC(50) < 1.1 muM) with no cytotoxicity (CC(50) > 25 muM). In addition, both compounds showed acceptable results in metabolic stabilities, hERG binding affinities, CYP inhibitions, and preliminary PK studies.
  • |*Drug Design[MESH]
  • |Animals[MESH]
  • |Antiviral Agents/*chemical synthesis/pharmacokinetics/pharmacology/therapeutic use[MESH]
  • |COVID-19 Drug Treatment[MESH]
  • |COVID-19/virology[MESH]
  • |Cell Line[MESH]
  • |Cell Survival/drug effects[MESH]
  • |Coronavirus Infections/drug therapy/virology[MESH]
  • |Cytochrome P-450 Enzyme System/chemistry/metabolism[MESH]
  • |Half-Life[MESH]
  • |Humans[MESH]
  • |Inhibitory Concentration 50[MESH]
  • |Mice[MESH]
  • |Microsomes/metabolism[MESH]
  • |Middle East Respiratory Syndrome Coronavirus/*drug effects/isolation & purification[MESH]
  • |Quinazolinones/chemistry/metabolism/*pharmacology/therapeutic use[MESH]
  • |Rats[MESH]
  • |SARS-CoV-2/*drug effects/isolation & purification[MESH]


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