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...

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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2020
Materias:
Article
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
Descripción
Sumario: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.

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