Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors |
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| Authors: | Ji Hye Yoon Jun Young Lee Jihye Lee Young Sup Shin Sangeun Jeon Dong Eon Kim Jung Sun Min Jong Hwan Song Seungtaek Kim Sunoh Kwon Young-hee Jin Min Seong Jang Hyoung Rae Kim Chul Min Park |
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| Affiliation: | 1. Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea;2. Respiratory Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea;3. Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea;4. Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea;5. Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea |
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| Abstract: | 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 (IC50 = 86 nM) and low toxicity (CC50 > 25 μM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good in vivo PK properties. |
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| Keywords: | Corresponding author. MERS-CoV RNA virus Inhibitor SAR optimization |
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