Synthesis of Antidotes and Prophylactics for Organophosphorus Acetylcholinesterase Inhibitors
Abstract
Work has been completed on a series of w-carbamoyloxy-alkylimidazoles which are substituted at N1, C2 and C4 of the imidazole ring having chain lengths 1-3. All the N,N-dimethyl derivatives and representative N-methyl derivatives have been prepared. Work is continuing on a series of 5-,6-,7-and 8- substituted carbamoyloxy imidazo(1,2-a)pyridines. The 8-substituted series has been prepared for R(2) = H-, CH3-, (CH3)(2)CH- and Ph-. Work is in progress on the 5- and 6-substituted series and planned for the 7-substituted series. A total of 14 compounds have been submitted and 3 are in the final stages of preparation. In vitro acetycholinesterase inhibition data has been obtained for the w-carbamoyloxyalkylimidazoles. The 1-substituted compounds do not appear to be active but the 2- and 4-substituted series show modest activity. Excellent in vitro activity was observed for two previously submitted enol carbamates derived from 1,1-dimethyl-3-hydroxy-delta 3,4-piperidine.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jun 30, 1994
- Accession Number
- ADB188021
Entities
People
- Phuoc Van Nguyen
- Richard J. Sundberg
Organizations
- University of Virginia