Author: Young Lee, Jun; Sup Shin, Young; Lee, Jihye; Kwon, Sunoh; Jin, Young-hee; Seong Jang, Min; Kim, Seungtaek; Hwan Song, Jong; Rae Kim, Hyoung; Min Park, Chul
Title: Identification of 4-Anilino-6-aminoquinazoline Derivatives as Potential MERS-CoV Inhibitors Cord-id: x61eqaca Document date: 2020_8_8
ID: x61eqaca
Snippet: 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 an
Document: 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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