J. Lee, Y. Shin, Jihye Lee
Aug 8, 2020
Citations
0
Influential Citations
5
Citations
Journal
Bioorganic & Medicinal Chemistry Letters
Abstract
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.