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Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors
New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N(4)-(3-Chloro-4-fluorophenyl)-N(6)-(3-methoxybenzyl)quinazoline-4,6-diamine (1) has been identified in a random sc...
| Autores principales: | , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Elsevier Ltd.
2020
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7414322/ https://www.ncbi.nlm.nih.gov/pubmed/32781216 http://dx.doi.org/10.1016/j.bmcl.2020.127472 |
| _version_ | 1783568952563073024 |
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| author | Lee, Jun Young Shin, Young Sup Lee, Jihye Kwon, Sunoh Jin, Young-hee Jang, Min Seong Kim, Seungtaek Song, Jong Hwan Kim, Hyoung Rae Park, Chul Min |
| author_facet | Lee, Jun Young Shin, Young Sup Lee, Jihye Kwon, Sunoh Jin, Young-hee Jang, Min Seong Kim, Seungtaek Song, Jong Hwan Kim, Hyoung Rae Park, Chul Min |
| author_sort | Lee, Jun Young |
| collection | PubMed |
| description | New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N(4)-(3-Chloro-4-fluorophenyl)-N(6)-(3-methoxybenzyl)quinazoline-4,6-diamine (1) has been identified in a random screen as a hit compound for inhibiting MERS-CoV infection. Throughout optimization process, compound 20 was found to exhibit high inhibitory effect (IC(50) = 0.157 μM, SI = 25) with no cytotoxicity and moderate in vivo PK properties. |
| format | Online Article Text |
| id | pubmed-7414322 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2020 |
| publisher | Elsevier Ltd. |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-74143222020-08-10 Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors Lee, Jun Young Shin, Young Sup Lee, Jihye Kwon, Sunoh Jin, Young-hee Jang, Min Seong Kim, Seungtaek Song, Jong Hwan Kim, Hyoung Rae Park, Chul Min Bioorg Med Chem Lett Article New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N(4)-(3-Chloro-4-fluorophenyl)-N(6)-(3-methoxybenzyl)quinazoline-4,6-diamine (1) has been identified in a random screen as a hit compound for inhibiting MERS-CoV infection. Throughout optimization process, compound 20 was found to exhibit high inhibitory effect (IC(50) = 0.157 μM, SI = 25) with no cytotoxicity and moderate in vivo PK properties. Elsevier Ltd. 2020-10-15 2020-08-08 /pmc/articles/PMC7414322/ /pubmed/32781216 http://dx.doi.org/10.1016/j.bmcl.2020.127472 Text en © 2020 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 Lee, Jun Young Shin, Young Sup Lee, Jihye Kwon, Sunoh Jin, Young-hee Jang, Min Seong Kim, Seungtaek Song, Jong Hwan Kim, Hyoung Rae Park, Chul Min Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors |
| title | Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors |
| title_full | Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors |
| title_fullStr | Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors |
| title_full_unstemmed | Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors |
| title_short | Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors |
| title_sort | identification of 4-anilino-6-aminoquinazoline derivatives as potential mers-cov inhibitors |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7414322/ https://www.ncbi.nlm.nih.gov/pubmed/32781216 http://dx.doi.org/10.1016/j.bmcl.2020.127472 |
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