Anti-Ebola Activity of Diazachrysene Small Molecules
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Gharaibeh, Dima N.
Šegan, Sandra B.
Panchal, Rekha G.
Šolaja, Bogdan A.
Article (Published version)
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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 mu M) 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.
Keywords:Ebola virus / antiviral diazachrysenes / inhibitory efficacy small molecule / toxicity
Source:ACS INFECTIOUS DISEASES, 2015, 1, 6, 264-271
- Amer Chemical Soc, Washington
- The synthesis of aminoquinoline-based antimalarials and botulinum neurotoxin A inhibitors (RS-172008)
- Department of Defense Chemical Biological Defense Program through Defense Threat Reduction Agency (DTRA)
- Supplementary material: http://cherry.chem.bg.ac.rs/handle/123456789/3339