Design and synthesis of benzodiazepine-1,2,3-triazole hybrid derivatives as selective butyrylcholinesterase inhibitors

Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

“…Foroumadi et al (2020) synthesized 1,2,3-triazole-containing 3-phenylcoumarin-lipoic acid conjugates which showed promising AChE and BChE activity, with IC 50 at the µM level. Compound 137 displayed excellent AChE (IC 50 = 7.3 µM) and BChE (IC 50 = 68.6 µM) activity, indicating that it may act as promising multi-functional agent for additional development 219 ( Table 5 ).…”

“…Additionally, molecular docking investigations indicated that the thiazolidinediones function plays a key part in the inhibition mechanism by well-tting into the enzyme binding pocket 218 (Table5).Foroumadi et al (2020) synthesized 1,2,3-triazole-containing 3-phenylcoumarin-lipoic acid conjugates which showed promising AChE and BChE activity, with IC 50 at the mM level. Compound 137 displayed excellent AChE (IC 50 ¼ 7.3 mM) and BChE (IC 50 ¼ 68.6 mM) activity, indicating that it may act as promising multi-functional agent for additional development219 (Table…”

Chalcone derived benzoheterodiazepines for medicinal applications: A Two‐pot and one‐pot synthetic approach

“…promising biological properties. Triazole incorporated benzodiazepines have been reported with excellent butyrylcholinesterase inhibitors [133]. Triazole is a vital bioactive compound due to the existence of two H-bond acceptors that able to form stable adduct via π-π stacking, dipole interaction, and H-bonding with the target molecules to improve the pharmacokinetic properties.…”

Design, Synthesis, and biological evaluation of pyrazolo-benzothiazole derivatives as a potential therapeutic agent for the treatment of Alzheimer’s disease

“…[8] The pharmacological agents approved for AD management have some bene cial effects on cognitive, and behavioral symptoms of the disease, however, these agents do not play any role to address basic aspects of the disease. [9] Moreover, these agents are neuro-destructive rather than having neuroprotective effect.…”