Anti-Ebola Activity of Diazachrysene Small Molecules.
Herein we report on a diazachrysene class of small molecules that exhibit potent antiviral activity against the Ebola (EBOV) virus. The antiviral compounds are easily synthesized, and the most active compounds have excellent in vitro activity (0.34-0.70 μM) and are significantly less lipophilic than their predecessors. The three most potent diazachrysene antivirals do not exhibit any toxicity in vivo and protected 70-90% of the mice at 10 mg/kg following EBOV challenge. Together, these studies suggest that diazachrysenes are a promising class of compounds for hit to lead optimization and as potential Ebola therapeutics.
Faculty of Chemistry, University of Belgrade , Studentski trg 16, P.O. Box 51, 11158 Belgrade, Serbia.
Života
Ž
Selaković
United States Army Medical Research Institute of Institute of Infectious Diseases, Fort Detrick, 1425 Porter Street, Frederick, Maryland 21702, United States.
Veronica
V
Soloveva
United States Army Medical Research Institute of Institute of Infectious Diseases, Fort Detrick, 1425 Porter Street, Frederick, Maryland 21702, United States.
Dima N
DN
Gharaibeh
United States Army Medical Research Institute of Institute of Infectious Diseases, Fort Detrick, 1425 Porter Street, Frederick, Maryland 21702, United States.
Jay
J
Wells
Faculty of Chemistry, University of Belgrade , Studentski trg 16, P.O. Box 51, 11158 Belgrade, Serbia.
Sandra
S
Šegan
United States Army Medical Research Institute of Institute of Infectious Diseases, Fort Detrick, 1425 Porter Street, Frederick, Maryland 21702, United States.
Rekha G
RG
Panchal
Faculty of Chemistry, University of Belgrade , Studentski trg 16, P.O. Box 51, 11158 Belgrade, Serbia.
Bogdan A
BA
Šolaja
Ebola virus; antiviral diazachrysenes; inhibitory efficacy small molecule; toxicity