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DDX3X Helicase Inhibitors as a New Strategy To Fight the West Nile Virus Infection.

Authors :
Brai A
Martelli F
Riva V
Garbelli A
Fazi R
Zamperini C
Pollutri A
Falsitta L
Ronzini S
Maccari L
Maga G
Giannecchini S
Botta M
Source :
Journal of medicinal chemistry [J Med Chem] 2019 Mar 14; Vol. 62 (5), pp. 2333-2347. Date of Electronic Publication: 2019 Feb 21.
Publication Year :
2019

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.

Details

Language :
English
ISSN :
1520-4804
Volume :
62
Issue :
5
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
30721061
Full Text :
https://doi.org/10.1021/acs.jmedchem.8b01403