Synthesis, characterization, crystal structure and biological evaluation of 1,3,5-triazine-quinoline derivatives as butyrylcholinesterase inhibitors

Recent biological applications of heterocyclic hybrids containing s-triazine scaffold

“…This heterocyclic compound was linked with striazine to form 16 new s-triazine-quinoline molecular hybrids (73). 87 Using colorimetric Ellman's method, synthesized compounds were screened for their cholinesterase inhibition activity, SAR suggested that when R 1 is pyrrolidine and R 2 the linker between s-triazine and quinoline is piperidin-3ylmethanamine, the anti-Alzheimer potency is remarkably enhanced than any other amino group present as the linker and the IC 50 value was noted to be hAChE = 10.82 ± 0.98 mM and hBuChE = 0.046 ± 0.002 mM. Docking analysis suggested that this compound can interact with and block the active site of butyrylcholinesterase (Table 4).…”

Design, synthesis and evaluation of N-arylmethylamide derivatives as cholinesterase inhibitors

“…However, butyrylcholinesterase (BuChE) in the brain of advanced AD was found to 165% higher than normal level [18,19], which can also hydrolyze ACh [20]. Thereby, butyrylcholinesterase inhibitors (BuChEIs) may be used to treat advanced AD, and by now, many novel BuChEIs for the treatment of AD have been reported, such as compounds 8-10 [22][23][24] (Fig. 2).…”

“…With the in-depth study on AD, it was found that AChE is the main enzyme responsible for ACh metabolism in the normal brain and in the early stages of AD [17], but the AChE is 67% lower than normal level in stages of advanced AD, which lead to lose e cacy of AChEIs for treating advanced AD. However, butyrylcholinesterase (BuChE) in the brain of advanced AD was found to 165% higher than normal level [18,19], which can also hydrolyze ACh [20].…”