Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors.

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.

SUBMITTER: Lee JY 

PROVIDER: S-EPMC7414322 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature