A limited structural modification results in a significantly more efficacious diazachrysene-based filovirus inhibitor.

ABSTRACT: Ebola (EBOV) and Marburg (MARV) filoviruses are highly infectious pathogens causing deadly hemorrhagic fever in humans and non-human primates. Promising vaccine candidates providing immunity against filoviruses have been reported. However, the sporadic nature and swift progression of filovirus disease underlines the need for the development of small molecule therapeutics providing immediate antiviral effects. Herein we describe a brief structural exploration of two previously reported diazachrysene (DAAC)-based EBOV inhibitors. Specifically, three analogs were prepared to examine how slight substituent modifications would affect inhibitory efficacy and inhibitor-mediated toxicity during not only EBOV, but also MARV cellular infection. Of the three analogs, one was highly efficacious, provi

SUBMITTER: Selakovic Z 

PROVIDER: S-EPMC3446762 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature