Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors |
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| Affiliation: | 1. Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea;2. Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea;3. Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea;4. KM Application Center, Korea Institute of Oriental Medicine, Dong-gu, Daegu 41062, South Korea;5. Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea |
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| 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. |
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| Keywords: | MERS-CoV 4-Anilino-6-aminoquinazoline Coronavirus Inhibitor Optimization |
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