| Literature DB >> 30721061 |
Annalaura Brai1,2, Francesco Martelli3, Valentina Riva4, Anna Garbelli4, Roberta Fazi1, Claudio Zamperini1,2, Alessandro Pollutri1, Lucia Falsitta1, Stefania Ronzini1, Laura Maccari2, Giovanni Maga4, Simone Giannecchini3, Maurizio Botta1,2,5.
Abstract
Increased frequency of arbovirus outbreaks in the last 10 years represents an important emergence for global health. Climate warming, extensive urbanization of tropical regions, and human migration flows facilitate the expansion of anthropophilic mosquitos and the emerging or re-emerging of new viral infections. Only recently the human adenosinetriphosphatase/RNA helicase X-linked DEAD-box polypeptide 3 (DDX3X) emerged as a novel therapeutic target in the fight against infectious diseases. Herein, starting from our previous studies, a new family of DDX3X inhibitors was designed, synthesized, validated on the target enzyme, and evaluated against the West Nile virus (WNV) infection. Time of addition experiments after virus infection indicated that the compounds exerted their antiviral activities after the entry process, likely at the protein translation step of WNV replication. Finally, the most interesting compounds were then analyzed for their in vitro pharmacokinetic parameters, revealing favorable absorption, distribution, metabolism, and excretion values. The good safety profile together with a good activity against WNV for which no treatments are currently available, make this new class of molecules a good starting point for further in vivo studies.Entities:
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Year: 2019 PMID: 30721061 DOI: 10.1021/acs.jmedchem.8b01403
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446