Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors.
Bioorg Med Chem Lett
; 30(20): 127472, 2020 10 15.
Article
em En
| MEDLINE
| ID: mdl-32781216
ABSTRACT
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. N4-(3-Chloro-4-fluorophenyl)-N6-(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 (IC50 = 0.157 µM, SI = 25) with no cytotoxicity and moderate in vivo PK properties.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Quinazolinas
/
Coronavírus da Síndrome Respiratória do Oriente Médio
/
Compostos de Anilina
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article