engleski

Evaluation of Biological Activity of New Guanidinium Based Adamantane Compounds Novel Adamantane Derivatives as Potent Butyrylcholinesterase Inhibitors

It is known that the adamantane moiety plays an important biological role in various types of compounds due to its lipophilicity and bulkiness.[1] These findings suggest the importance of the adamantane substructure to reach and interact with the site of activity. On the other hand, the compounds with an incorporated guanidinium moiety are also known to act as pharmacologically active substrates with antimicrobial [2], antiviral [3] and anti- cancer action [4]. Polycyclic guanylhydrazones have recently found application as nitric oxide synthase (NOS) inhibitors.[5] In our recent study we have tried to combine the effects of these two subunits hoping for a synergic result. We have successfully synthesized adamantane guanylhydrazones 1-5 and have tested them as butyrylcholinesterase inhibitors. The inhibition of liophylized horse serum butyrylcholinesterase by compounds 1-5 was measured with acetylthiocholine as substrate. The Ellman's method [6] for cholinesterase activity determination was used and the inhibition constants were determined using the Hunter and Downs diagrams. The obtained results were supported with docking studies.

adamantane ; inhibitors ; butyrylcholinesterase ; kinetic and docking studies

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