The threat to human health posed by anthrax highlights the need for identifying effective ways to combat this fatal disease. Current treatment options are limited to a small number of antibiotics but these fail to eliminate or prevent damage due to anthrax-related toxin. A vital step in anthrax poisoning is proteolytic activation of Protective Antigen (PA) by human cellular proteases. The goal of this project is to synthesize a small molecule library with the potential to bind PA and block its proteolytic activation by furin. We report the concise syntheses of 24 structurally diverse agents.

Progress towards structure-based <i>de novo</i> design and synthesis of small molecule inhibitors of protective antigen (PA): An anti-toxin approach for combating anthrax

251st National Meeting (2016)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.

Progress towards structure-based de novo design and synthesis of small molecule inhibitors of protective antigen (PA): An anti-toxin approach for combating anthrax