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10.1016/j.bmcl.2020.127472

http://scihub22266oqcxt.onion/10.1016/j.bmcl.2020.127472
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32781216!7414322!32781216
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suck abstract from ncbi


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pmid32781216      Bioorg+Med+Chem+Lett 2020 ; 30 (20): 127472
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  • Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors #MMPMID32781216
  • Lee JY; Shin YS; Lee J; Kwon S; Jin YH; Jang MS; Kim S; Song JH; Kim HR; Park CM
  • Bioorg Med Chem Lett 2020[Oct]; 30 (20): 127472 PMID32781216show ga
  • New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N(4)-(3-Chloro-4-fluorophenyl)-N(6)-(3-methoxybenzyl)quinazoline-4,6-diamine (1) has been identified in a random screen as a hit compound for inhibiting MERS-CoV infection. Throughout optimization process, compound 20 was found to exhibit high inhibitory effect (IC(50) = 0.157 muM, SI = 25) with no cytotoxicity and moderate in vivo PK properties.
  • |Aniline Compounds/chemical synthesis/pharmacokinetics/*pharmacology/toxicity[MESH]
  • |Animals[MESH]
  • |Antiviral Agents/chemical synthesis/pharmacokinetics/*pharmacology/toxicity[MESH]
  • |Cell Line[MESH]
  • |Chlorocebus aethiops[MESH]
  • |Cricetulus[MESH]
  • |Humans[MESH]
  • |Mice[MESH]
  • |Microbial Sensitivity Tests[MESH]
  • |Middle East Respiratory Syndrome Coronavirus/*drug effects[MESH]
  • |Molecular Structure[MESH]
  • |Quinazolines/chemical synthesis/pharmacokinetics/*pharmacology/toxicity[MESH]
  • |Rats[MESH]


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