Synthesis of 2-aryl-4-(4-β-D-allopyranosyloxyphenyl)4,6,7,8-tetrahydroquinolin-5(1H)-one derivatives under solvent-free conditions and study of sedative activity
Under solvent-free conditions, syntheses of 2-aryl-4-(4-β-D-allopyranosyloxyphenyl)-4,6,7,8tetrahydroquinolin-5(1H)-one derivatives were carried out from chalcone (2a–2e), cyclohexane-1,3-dione (3), and NH4OAc in excellent yield without using any catalysts. The structure of the new compounds were characterized by 1H NMR, IR, and HR-MS spectroscopy. The preliminary bioassay tests of 4a–4j indicated that compounds 4b, 4e, and 4f exhibited potent sedative and hypnotic activity.
Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.
A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent AChE inhibitory activities with IC(50) values of 0.45+/-0.02microM, 0.49+/-0.02microM, and 0.20+/-0.01microM, respectively. High selectivity for AChE over BuChE was also observed. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type.
A numerical study on liquid ring motion and fragmentation for the initial process of liquid explosive dispersal
For the explosive dispersal on liquid fuel of FAE technique, the expansion of gaseous detonation products, axisymmetric radial extension and fragmentation of a liquid ring were analyzed, then corresponding models were established. By those models coupled, the numerical simulation on motion and fragmentation of the liquid ring exerted by strong action was carried out. The results computed show that the models established are feasible, and present study can offer initial conditions for the numerical simulation on the process of liquid secondary breakup and gas-liquid mixing.