Synthesis of Antidotes and Prophylactics for Organophosphorus Acetylcholinesterase Inhibitors
Abstract
New compounds were prepared for evaluation as antidotal and or prophylactic activity against toxic organophosphorus acetylcholinesterase inhibitors. One series of compounds consists of the 5-, 6-, 7-, and 8-(N,N-dimethylcarbamoyloxy) derivatives of 1-methylimidazo(1,2-a)pyridinium ion with varying C2 substituents. Fifteen new compounds were prepared. These compounds show substantial activity as inhibitors of acetylcholinesterase (electric eel) but no data are available on in vivo protective activity. A second series of compounds included thirteen new carbamoyloxyalkylimidazolium salts. Some of these compounds show marginal activity as acetylcholinesterase inhibitors. The two lead compounds in this series had shown in vivo activity, but no in vivo data has been obtained for the new compounds. Five additional compounds including two phenols and three enol carbamates were prepared. The report includes synthetic methods, spectroscopic data and elemental analysis for all new compounds prepared.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jan 01, 1996
- Accession Number
- ADB211649
Entities
People
- Richard J. Sundberg
Organizations
- University of Virginia