3-Acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives were synthesized and evaluated to show high anti-MERS-CoV inhibitory activities. Among them, 6,8-difluoro-3-isobutyryl-2-((2,3,4-trifluorophenyl)amino)quinolin-4(1H)-one (6u) exhibits high inhibitory effect (IC = 86 nM) and low toxicity (CC > 25 μM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good in vivo PK properties.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126094 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2019.126727 | DOI Listing |
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