Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer’s disease

Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors

“…Similar activity was observed by Tasso [14] with quinolizidinyl derivatives of bi-and tricyclic structures.…”

Synthesis, spectroscopic characterization, photochemical and photophysical properties and biological activities of ruthenium complexes with mono- and bi-dentate histamine ligand

“…The IC 50 (50% AChE inhibitory effect) of (1R + 2A) was determined to be 21 μmol L . When compared to many commercially proven drugs in various countries to treat Alzheimer's disease we can affirm that this complex is an inhibitor that is nine times stronger than the commercial drug rivastigmine 26 2+ contributes to the inhibition of enzymes in a significant way.…”

Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives

“…At the mouth of the gorge, the π-π stacking interaction between the phenyl ring of the compounds and Tyr70 has been found. Additionally, in the middle of the gorge, the π-π stacking interaction has been observed between the coumarin and the benzene ring of Phe330 [15,16,20,21]. A hydrogen bond has also been formed between amid moieties of the compounds containing urea, carbamate or sulphonamide groups and Tyr70 and His447 [37][38][39][40].…”

“…The results showed that most of the synthesized compounds exhibited inhibitory activity against [4,20]. e31 exhibited the strongest inhibition against BuChE with IC 50 value of 4.93 µM, which was 3.5-fold more potent than that of galantamine (IC 50 = 17.38 µM).…”

“…Several studies have revealed that the tricycle and heterocyclic rings (such as tacrine, quinolizidinyl and coumarin derivatives) showed strong parallel π-π stacking against CAS, and the amidic or imidic fragments interact with the catalytic triad of the active site [18][19][20][21]. The coumarin heterocyclic framework is now considered as a privileged structure, which is a common moiety found in many biologically active natural and therapeutic products and thus represents a very important pharmacophore [22,23].…”