Li, Qi published the artcileHighly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection, Application In Synthesis of 332026-86-5, the publication is Journal of Medicinal Chemistry (2021), 64(10), 6856-6876, database is CAplus and MEDLINE.
Butyrylcholinesterase (BChE) has been considered as a potential therapeutic target for Alzheimer’s disease (AD) because of its compensation capacity to hydrolyze acetylcholine (ACh) and its close association with Aβ deposit. Here, we identified S06-1011 (hBChE IC50 = 16 nM) and S06-1031 (hBChE IC50 = 25 nM) as highly effective and selective BChE inhibitors, which were proved to be safe and long-acting. Candidate compounds exhibited neuroprotective effects and the ability to improve cognition in scopolamine- and Aβ1-42 peptide-induced cognitive deficit models. The best candidate S06-1011 increased the level of ghrelin, a substrate of BChE, which can function as improving the mental mood appetite. The weight gain of the S06-1011-treated group remarkably increased. Hence, BChE inhibition not only plays a protective role against dementia but also exerts a great effect on treating and nursing care.
Journal of Medicinal Chemistry published new progress about 332026-86-5. 332026-86-5 belongs to imidazoles-derivatives, auxiliary class Oxadiazole,Amine,Benzimidazole, name is 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, and the molecular formula is C9H7N5O, Application In Synthesis of 332026-86-5.
Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem