Synthesis and biological evaluation of new oxopyrrolidine derivatives as inhibitors of acetyl cholinesterase and β amyloid protein as anti – Alzheimer’s agents

Synthesis, and molecular modeling of bis(3-(piperazine-1-yl)propyl)tungstate (BPPT) nanoparticles, and its first catalytic application for one-pot synthesis of 4H-chromene derivatives

“…The containing of alkylamine side chain in BPPT chemical structure and considering the structures of drugs that inhibit acetylcholinesterase enzyme such as donepezil, and rivastigmine (used for the treatment of Alzheimer, Parkinson, and Autism), and also other potent acetylcholinesterase inhibitors that have contained piperidine or piperazine side chains in their structures (Liu et al., 2018a; Mohamed et al., 2018), we decided to study molecular docking for BPPT, and compare the results with the Donepezil as reference drug to treatment of Alzheimer (Fig. 9).…”

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

“…Most compounds showed decent inhibitory ability where compound 173 garnered the highest activity against AChE with IC 50 value 1.84 ng g −1 tissue compared to the standard donepezil 3.34 ng g −1 tissue. Furthermore, compound 174 displayed the greatest activity against β-42 protein with IC 50 value of 11.3 Pg g −1 tissue compared to 18.4 Pg g −1 tissue of donepezil 241 ( Table 7 ).…”

Beta and Gamma Amino Acid-Substituted Benzenesulfonamides as Inhibitors of Human Carbonic Anhydrases

“…Compound 25b also had an unusually strong interaction with CAIII (K d_obs 5000 nM, Table 2), despite having large substituents, which usually contribute to steric hindrance and weak binding to CAIII. (27)(28)(29)(30)(31)(32)(33)(34)(35)(36) Binding to CA Compounds 27-6 had greater asymmetry than compounds 2-25a,b (Figure 3). Compounds 27-34 and 36 were tested with all catalytically active CA isozymes.…”

“…Light-brown solid, yield 0.17 g (71%); m.p. 151-152 • C; IR (KBr) (v, cm −1 ): 3308, 3241, 3078; 1 H NMR (400 MHz, DMSO-d 6 ) δ (ppm): 3.15-3.22 (m, 2H, CH 2 ), 3.36, 3.40 (2s, 6H, 2CH 3 ), 3.57-3.67 (m, 2H, NCH 2 ), 3.71-3.83 (m, 1H, CH), 6.39 (t, 1H, J = 6.1 Hz, ArNH), 6 (27) Carboxylic acid 26 (0.45 g, 1.5 mmol) and NaOAc (0.20 g, 2.5 mmol) were dissolved into 10 mL of hot water. Then, chloroacetone (0.20 mL, 2.5 mmol) was added, and reaction mixture was heated at reflux for 4h.…”

“…The 5-oxopyrrolidine moiety is a part of a variety of compounds of natural or synthetic origin [26,27]. Recently, we have synthesized and examined the binding properties of 3-substituted 1-(4-sulfamoylphenyl)-5-oxopyrrolidine derivatives [28][29][30].…”