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Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors
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 toxic...
| Autores principales: | , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Elsevier Ltd.
2019
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126094/ https://www.ncbi.nlm.nih.gov/pubmed/31624041 http://dx.doi.org/10.1016/j.bmcl.2019.126727 |
| _version_ | 1783516074940039168 |
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| 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 |
| author_facet | 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 |
| author_sort | Yoon, Ji Hye |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-7126094 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2019 |
| publisher | Elsevier Ltd. |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-71260942020-04-08 Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors 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 Bioorg Med Chem Lett Article 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. Elsevier Ltd. 2019-12-01 2019-10-09 /pmc/articles/PMC7126094/ /pubmed/31624041 http://dx.doi.org/10.1016/j.bmcl.2019.126727 Text en © 2019 Elsevier Ltd. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active. |
| spellingShingle | Article 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 Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors |
| title | Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors |
| title_full | Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors |
| title_fullStr | Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors |
| title_full_unstemmed | Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors |
| title_short | Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors |
| title_sort | synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1h)-one derivatives as potential mers-cov inhibitors |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126094/ https://www.ncbi.nlm.nih.gov/pubmed/31624041 http://dx.doi.org/10.1016/j.bmcl.2019.126727 |
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