Author: Yoon, Ji Hye; Lee, Jun Young; Lee, Jihye; Shin, Young Sup; Jeon, Sangeun; Kim, Dong Eon; Min, Jung Sun; Song, Jong Hwan; Kim, Seungtaek; Kwon, Sunoh; Jin, Young-hee; Jang, Min Seong; Kim, Hyoung Rae; Park, Chul Min
Title: Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors Cord-id: hlekc96l Document date: 2019_12_1
ID: hlekc96l
Snippet: 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(50) = 86 nM) and low toxicity (CC(50) > 25 μM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good in vivo PK properties.
Document: 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(50) = 86 nM) and low toxicity (CC(50) > 25 μM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good in vivo PK properties.
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