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Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Dec 01; Vol. 29 (23), pp. 126727. Date of Electronic Publication: 2019 Oct 09. - Publication Year :
- 2019
-
Abstract
- 3-Acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives were synthesized and evaluated to show high anti-MERS-CoV inhibitory activities. Among them, 6,8-difluoro-3-isobutyryl-2-((2,3,4-trifluorophenyl)amino)quinolin-4(1H)-one (6u) exhibits high inhibitory effect (IC <subscript>50</subscript> = 86 nM) and low toxicity (CC <subscript>50</subscript> > 25 μM). Moreover, it shows good metabolic stability, low hERG binding affinity, no cytotoxicity, and good in vivo PK properties.<br /> (Copyright © 2019 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Antiviral Agents chemical synthesis
Antiviral Agents chemistry
CHO Cells
Cell Survival drug effects
Chlorocebus aethiops
Cricetulus
Dose-Response Relationship, Drug
Humans
Mice
Microbial Sensitivity Tests
Molecular Structure
NIH 3T3 Cells
Quinolones chemical synthesis
Quinolones chemistry
Structure-Activity Relationship
Vero Cells
Antiviral Agents pharmacology
Middle East Respiratory Syndrome Coronavirus drug effects
Quinolones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 31624041
- Full Text :
- https://doi.org/10.1016/j.bmcl.2019.126727