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Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Bioorg+Med+Chem+Lett 2021 ; 39 (ä): 127885 Nephropedia Template TP
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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.