Benzimidazole-Carboxamides as Potential Therapeutics for Alzheimer’s Disease: Primary Analysis In Silico and In Vitro

A primary in vitro analysis of the anticholinesterase properties of substituted 1,3-dihydro-2-oxo-1 H -benzimidazol-2-ones was performed along with in silico calculation of their oral toxicity. These compounds are analogs of BIMU-8, a well-known agonist of serotonin 5-HT 4 receptors, and are suppose...

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Veröffentlicht in:Bulletin of experimental biology and medicine 2023-07, Vol.175 (3), p.345-352
Hauptverfasser: Chelusnova, Yu.V., Voronina, P. A., Belinskaia, D. A., Goncharov, N. V.
Format: Artikel
Sprache:eng
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Zusammenfassung:A primary in vitro analysis of the anticholinesterase properties of substituted 1,3-dihydro-2-oxo-1 H -benzimidazol-2-ones was performed along with in silico calculation of their oral toxicity. These compounds are analogs of BIMU-8, a well-known agonist of serotonin 5-HT 4 receptors, and are supposed to combine the functions of cholinesterase inhibitors and serotonin receptor agonists. Biochemical analysis showed the ability of the obtained chemicals to inhibit acetyl- and butyrylcholinesterase. A compound with minimal toxicity, high inhibitory ability against butyrylcholinesterase, and low inhibitory ability against acetylcholinesterase has been identified, which is of greatest interest for further experimental development.
ISSN:0007-4888
1573-8221
1573-8221
DOI:10.1007/s10517-023-05865-4