Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines.
Basic Information
ID: ALA4725262
Journal: Bioorg Med Chem Lett
Title: Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines.
Authors: Saul S,Pu SY,Zuercher WJ,Einav S,Asquith CRM
Abstract: Screening a series of 4-anilinoquinolines and 4-anilinoquinazolines enabled identification of potent novel inhibitors of dengue virus (DENV). Preparation of focused 4-anilinoquinoline/quinazoline scaffold arrays led to the identification of a series of high potency 6-substituted bromine and iodine derivatives. The most potent compound 6-iodo-4-((3,4,5-trimethoxyphenyl)amino)quinoline-3-carbonitrile (47) inhibited DENV infection with an EC = 79 nM. Crucially, these compounds showed very limited toxicity with CC values >10 µM in almost all cases. This new promising series provides an anchor point for further development to optimize compound properties.
CiteXplore: 32631507
DOI: 10.1016/j.bmcl.2020.127284
Patent ID: ┄