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 |
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Hauptverfasser: | , , , |
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. |
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ISSN: | 0007-4888 1573-8221 1573-8221 |
DOI: | 10.1007/s10517-023-05865-4 |