Bridged Bicyclic Systems as Acetylcholinesterase Reactivators and Pretreatment Drugs.

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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.

Author(s):
Moriarty, Robert M.
Author Organization(s):
ILLINOIS UNIV AT CHICAGO CIRCLE
Descriptive Note:
Annual rept. 15 Jul 87-14 Jul 88,
Pagination:
0057

Security Markings

DOCUMENT & CONTEXTUAL SUMMARY

Distribution:
Approved For Public Release
Distribution Statement:
Approved For Public Release; Distribution Unlimited.

RECORD

Collection: TR
Identifying Numbers
Contract/Grant Number(s):
DAMD17-85-C-5190
Task Number(s):
AJ
Project Number(s):
3M162734A875
Monitor Series:
USAMRDC
 Subject Terms
Communities of Interest:
No COI(s) Identified
Descriptor(s):
, ACETYLCHOLINESTERASE, ANIMALS, DRUGS, IN VITRO ANALYSIS, IN VIVO ANALYSIS, INHIBITION, IRREVERSIBLE PROCESSES, REVERSIBLE, TEST AND EVALUATION
Field(s)/Group(s):
Biochemistry, Organic Chemistry
Keyword(s):
Bridged bicyclic oximes, Acetylcholinesterase, Acetylcholinesterase reactivators, Tropane, Atropine analogs, PE62734A, WU108, AS875
Report Date:
1990 Jan 15