Accession Number:

ADB211649

Title:

Synthesis of Antidotes and Prophylactics for Organophosphorus Acetylcholinesterase Inhibitors

Descriptive Note:

Final rept. 1 Jun 92-31 Dec 95

Corporate Author:

VIRGINIA UNIV CHARLOTTESVILLE

Personal Author(s):

Report Date:

1996-01-01

Pagination or Media Count:

62.0

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-methylimidazo1,2-apyridinium 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.

Subject Categories:

  • Biochemistry
  • Toxicology

Distribution Statement:

APPROVED FOR PUBLIC RELEASE