Inhibitory effect of benzimidazole derivatives on cholinesterases of animals in the presence of different substrates

Specifically synthesized group of benzimidazole derivatives possessing varying degrees of delocalization of the positive charge in the cation group of the molecule has been studied in order to search for potential cholinergically active compounds and to study the role of the Coulomb interaction in c...

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Bibliographic Details
Published in:Ukrainian biochemical journal 2014-09, Vol.86 (5), p.47-55
Main Authors: Basova, N E, Kormilitsyn, B N, Perchenok, A Iu, Rosengart, E V, Saakov, V S, Suvorov, A A
Format: Article
Language:eng ; rus
Subjects:
Acetylthiocholine - analogs & derivatives
Acetylthiocholine - chemistry
Animals
benzimidazol reversible inhibitors
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Brain Chemistry
Cholinesterase Inhibitors - chemical synthesis
Cholinesterase Inhibitors - chemistry
Cholinesterase Inhibitors - pharmacology
Cholinesterases - chemistry
Cholinesterases - isolation & purification
cholinesterases of animals
Decapodiformes
Erythrocytes - chemistry
Erythrocytes - enzymology
Ganglia, Sensory - chemistry
Ganglia, Sensory - enzymology
Horses
Humans
Kinetics
Rana temporaria
Static Electricity
Structure-Activity Relationship
Substrate Specificity
substrates
Thiocholine - analogs & derivatives
Thiocholine - chemistry
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Summary:Specifically synthesized group of benzimidazole derivatives possessing varying degrees of delocalization of the positive charge in the cation group of the molecule has been studied in order to search for potential cholinergically active compounds and to study the role of the Coulomb interaction in cholinesterase catalysis. These compounds were reversible inhibitors of cholinesterase (ChE) of human erythrocytes, horse serum, brain of the frog Rana temporaria and visual ganglia of the Pacific squid Todarodes pacificus in the presence of acetylthiocholine iodide and propionylthiocholine iodide as substrates. The differences in the nature of reversible inhibitory effect were observed. The effect of the inhibitor structure and substrate nature, specific for each of the studied inhibitors, on the character of the process of reversible inhibition was found.
ISSN:2409-4943
2413-5003
DOI:10.15407/ubj86.05.047