Accession Number : ADB151091

Title :   Bridged Bicyclic Systems as Acetylcholinesterase Reactivators and Pretreatment Drugs.

Descriptive Note : Annual rept. 15 Jul 87-14 Jul 88,

Corporate Author : ILLINOIS UNIV AT CHICAGO CIRCLE

Personal Author(s) : Moriarty, Robert M.

Report Date : 15 JAN 1990

Pagination or Media Count : 57

Abstract : During the past year a variety of O-(N-substituted carbamoyl)-3-tropinone oximes, their methiodides and methchlorides have been synthesized and completely characterized. Optically active O-(N-a-methylbenzyl carbamoyl)-3-tropinone oxime methiodides methchlorides have also been synthesized in order to determine stereoselectivity. The synthesis of 8-N,N-tri and tetramethylene bis-O-(N-Methylcarbamoyl-3-tropinone oxime methiodides) have been achieved. These compounds have been submitted for testing. 8-N,N-Tetramethylene bis-(3-oximino-3-tropinone methiodide) has been synthesized and characterized. Animal test has been obtain for the compounds synthesized. Reversible inhibition, (KI), irreversible inhibition, k2 and KM for these compounds have been determined and a relationship has been discovered between in vitro and in vivo activity.

Descriptors :   , ACETYLCHOLINESTERASE, ANIMALS, DRUGS, IN VITRO ANALYSIS, IN VIVO ANALYSIS, INHIBITION, IRREVERSIBLE PROCESSES, REVERSIBLE, TEST AND EVALUATION.

Subject Categories : Biochemistry
      Organic Chemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE