Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors. Issue 20 (15th October 2020)

• Record Type: Journal Article
• Authors: Lee, Jun Young; Shin, Young Sup; Lee, Jihye; Kwon, Sunoh; Jin, Young-hee; Jang, Min Seong; Kim, Seungtaek; Song, Jong Hwan; Kim, Hyoung Rae; Park, Chul Min
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 20(2020)
• Publication Date: 2020-10-15
• Subjects: MERS-CoV -- 4-Anilino-6-aminoquinazoline -- Coronavirus -- Inhibitor -- Optimization; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.127472
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical 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. 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 (IC50 = 0.157 μM, SI = 25) with no cytotoxicity and moderate in vivo PK properties.