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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 ?M, SI = 25) with no cytotoxicity and moderate in vivo PK properties.

SUBMITTER: Lee JY

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

REPOSITORIES: biostudies-literature

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

Lee Jun Young JY Shin Young Sup YS Lee Jihye J Kwon Sunoh S Jin Young-Hee YH Jang Min Seong MS Kim Seungtaek S Song Jong Hwan JH Kim Hyoung Rae HR Park Chul Min CM

Bioorganic & medicinal chemistry letters 20200808 20

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 = 2 ...[more]

PMID: 32781216

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