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

摘要

A primary in vitro analysis of the anticholinesterase properties of substituted 1,3-dihydro-2-oxo-1H-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-HT4 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.