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Bioorg Med Chem Lett ; 52: 128407, 2021 11 15.
Article in English | MEDLINE | ID: mdl-34624490

ABSTRACT

There is an urgent need for novel strategies for the treatment of emerging arthropod-borne viral infections, including those caused by dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV). We prepared and screened focused libraries of 4-anilinoquinolines and 4-anilinoquinazolines for antiviral activity and identified three potent compounds. N-(2,5-dimethoxyphenyl)-6-(trifluoromethyl)quinolin-4-amine (10) inhibited DENV infection with an EC50 = 0.25 µM, N-(3,4-dichlorophenyl)-6-(trifluoromethyl)quinolin-4-amine (27) inhibited VEEV with an EC50 = 0.50 µM, while N-(3-ethynyl-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine (54) inhibited VEEV with an EC50 = 0.60 µM. These series of compounds demonstrated nearly no toxicity with CC50 values greater than 10 µM in all cases. These promising results provide a future prospective to develop a clinical compound against these emerging viral threats.


Subject(s)
Aniline Compounds/pharmacology , Antiviral Agents/pharmacology , Dengue Virus/drug effects , Encephalitis Virus, Venezuelan Equine/drug effects , Quinazolines/pharmacology , Aniline Compounds/chemical synthesis , Aniline Compounds/chemistry , Antiviral Agents/chemical synthesis , Antiviral Agents/chemistry , Dose-Response Relationship, Drug , Microbial Sensitivity Tests , Molecular Structure , Quinazolines/chemical synthesis , Quinazolines/chemistry , Structure-Activity Relationship
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