Accession Number:

ADA250681

Title:

Anticholinesterase Activity of Potential Therapeutic 5-(1,3,3- Trimethylindolinyl) Carbamates

Descriptive Note:

Corporate Author:

ARMY MEDICAL RESEARCH INST OF CHEMICAL DEFENSE ABERDEEN PROVING GROUND MD

Report Date:

1991-01-01

Pagination or Media Count:

10.0

Abstract:

Six N-alkyl and N-aryl 5-1,3,3-trimethylindolinyl carbamates were synthesized and studied for their structure-activity relationships in inhibiting eel acetylcholinesterase AChE. The carbamates were 5-1,3,3, trimethylindolinylN,N-dimethylcarbamate Cui Xing Ning I, 5-1,3,3- trimethylindolinylN-methylcarbamate II, 5-1,3,3-trimethylindolinylN- ethylcarbamate III, 5-1,3,3-trimethylindolinylN,Ndiethylcarbamate IV, 5- 1,3,3-trimethylindolinylN-heptylcarbamate V, and 5-1,3,3- trimethylindolinyl N-3-cholorophenylcarbamate VI. The inhibition studies were carried out at 25.0 deg C at pH 7.60. The rank order of the ki values for eel AChE inhibition is 11 V I Ill Vi IV. Compound 11 has a greater affinity for the enzyme than any irreversible inhibitor cited in the literature Kd 7.14 x 10-8M. Our findings should aid in the application of these carbamates 1 for counteracting the cholinergic problems associated with various diseases, and 2 for developing potential pretreatment compounds for organophosphate poisoning. Acetylcholinesterase, carbamates, inhibition

Subject Categories:

  • Biochemistry
  • Toxicology
  • Pharmacology

Distribution Statement:

APPROVED FOR PUBLIC RELEASE