ISSN:
0018-019X
Keywords:
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
The synthesis and characterization of some reversible acetylcholinesterase inhibitors are described in detail. They are structurally related to the natural substrate acetylcholine. All of them bear a trimethylammonium moiety as ‘cationic head’. Instead of an electrophilic ester group, the title compounds include a variety of functionalities, such as halide, ether, thioether, epoxide, amide, ketone and a double bond. The substances are thus suited as probes for the investigation of the esteratic subsite of the acetylcholinesterase active center.Most of the synthesized compounds inhibit the enzyme in a competitive manner with inhibition constants in the range of 10-5 M to 10-3 M. With respect to acetylcholine (KD ≤ 10-5 M and Km = (1.6±0.5) 10-4 M) their affinity to acetylcholinesterase is in the same order of magnitude.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/hlca.19830660731
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