Discovery of novel potent and low toxicity antiviral therapeutics targeting host factors, remains an active area in the field of medicinal chemistry. To initiate an in-house antiviral program against host-catalyzed capsid assembly pathways, we started screening our in-house compound collection and commercial libraries/ compounds using our proprietary screening assay involving de novo influenza protein biogenesis and assembly. Initial primary screening resulted in the identification of Pyrazole carboxamides with activities in the high nanomolar ranges against infectious influenza virus in cell culture. Optimization of the initial hit lead to the identification several highly potent antiviral compounds with good Pharmacokinetic properties has been achieved. The synthetic approaches and Structure Activity Relationships (SAR) will be presented.

Identification and lead optimization of pyrazole carboxamides with antiviral activity

253rd National Meeting (2017)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.