Li, Qi published the artcileDiscovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor, Recommanded Product: 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine, the publication is Journal of Medicinal Chemistry (2020), 63(17), 10030-10044, database is CAplus and MEDLINE.
To discover novel BChE inhibitors, a hierarchical virtual screening protocol followed by biochem. evaluation was applied. The most potent compound 8012-9656(I) (eqBChE IC50 = 0.18 ± 0.03 μM, hBChE IC50 = 0.32 ± 0.07 μM) was purchased and synthesized. It inhibited BChE in a noncompetitive manner and could occupy the binding pocket forming diverse interactions with the target. 8012-9656 was proven to be safe in vivo and in vitro and showed comparable performance in ameliorating the scopolamine-induced cognition impairment to tacrine. Addnl., treatment with 8012-9656 could almost entirely recover the Aβ1-42 (icv)-impaired cognitive function to the normal level and showed better behavioral performance than donepezil. The evaluation of the Aβ1-42 total amount confirmed its anti-amyloidogenic profile. Moreover, 8012-9656 possessed blood-brain barrier (BBB) penetrating ability, a long T1/2, and low intrinsic clearance. Hence, the novel potential BChE inhibitor 8012-9656 can be considered as a promising lead compound for further investigation of anti-AD agents.
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, Recommanded Product: 4-(1H-Benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine.
Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem