DESIGN AND SYNTHESIS OF POTENTIAL CHEMOTHERAPEUTIC COMPOUNDS FOR TREATING POISONING BY ANTICHOLINESTERASE COMPOUNDS, PREPARATION OF 5-SUBSTITUTED 2-PAM.
Abstract
Ten 5-substituted 2-PAM's were synthesized in 0.5- to 5.0-gm amounts for evaluation in therapy against anticholinesterase poisoning. Some preliminary studies of the protective effects of the benzyl, ethyl, methyl, and p-chlorobenzyloxy 2-PAM's (pyridino-2-adloxime methoiodides) conducted in vivo showed that the first three are approximately as effective as 2-PAMCl (pyridine-2-aldoxime methochloride) in promoting the survival of rabbits poisoned with GB. In in vitro experiments, however, all four were less effective than 2-PAMCl in reactivating the GB-inhibited red-blood-cell (RBC) cholinesterase of dogs. A more detailed evaluation of all compounds in this series will be made with the maximum dose that causes no symptoms. Additional compounds must be prepared to evaluate the premise that lipoid solubility may be important in the treatment or prophylaxis of anticholinesterase poisoning. (Author)
Document Details
- Document Type
- Technical Report
- Publication Date
- May 01, 1968
- Accession Number
- AD0832762
Entities
People
- Brennie E. Hackley Jr.
- Charles E. Johnson
- Lewis M. Berkowitz