engleski

3-Hydroxyquinuclidinium derivatives: synthesis and structures

It is known that compounds which contain quinuclidinium and imidazolium subunits possess a wide range of biological activities in the cholinergic system. Some of them were shown to be antidotes against organophosphorus, as well. In this work we describe the synthesis of N-methyl and N-(3-(2-hydrxyiminomethyl-3-methyl-1- imidazolio)-2-oxapropyl derivatives of 3-hydroxy, 3-dimethylcarbamoyloxy and 3-acetyloxy quinuclidines. Molecular modeling studies were undertaken in order to gain some insight on how different enantiomers of synthesized compounds might interact with acetylcholinesterase (AChE) binding sites. Synthesized quinuclidinium derivatives have been studied as reversible inhibitors of AChE and protectors against phosphorylation of the enzyme by some warfare agents.

3-Hydroxyquinuclidinium derivatives

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