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As N-alkyl-norlitebamines have been demonstrated to possess antiacetylcholinesterase activity, this study aimed to prepare related analogs to verify their structure-activity relationship. The compounds with the chemical skeletons of 2a-alkylnorlitebamines (6b-6e) and (7a,8)-didehydroisohomoaporphines (8b-8e, 9a, and 10b-10e) were designed and synthesized. In silico molecular docking of the 13 compounds on the acetylcholinesterase template indicated that 8a and 10b showed the highest docking scores (ΔG) (-20.56 Kcal/mol and -19.76 Kcal/mol, respectively). The reaction of peracylsecolaurolitsines under the modified Bischler-Napieralski procedure and subsequent NaBH4 reduction yielded 7a-alkyl-Bhomoaurolitsines 8a-8e, possessing a new skeleton, besides the expected 2a-alkyl-norlitebamines 10b-10e. Among these compounds, the two with the highest docking scores [Δ7a (8)-Bhomoaurolitsine (8a) and 2a-methyl-norlitebamine (10b)] showed better inhibitory activities against acetylcholin-esterase (eel) with IC50 value of 24.71 µM and 26.13 µM, respectively. Therefore, compounds 8a and 10b could serve as leads for exploring potential acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. [ABSTRACT FROM AUTHOR]

International projects are different from general domestic ones. In order to analyse the differences, a tripartite game model is built up to describe the relationship among owner, supervisor and general contractor, and some measures are given for the owner to more effectively complete the project. In addition, a project schedule selection model is formulated and a new benefit allocation method is proposed by introducing a new modified Shapley value with weighted factor. [ABSTRACT FROM PUBLISHER]

The effects on the physical and electro-optical properties of ferroelectric liquid crystals (FLCs) after the doping of a dilute suspension of ferroelectric nanoparticles (BaTiO3) have been studied. Due to the permanent electric dipole moments of the ferroelectric nanoparticles, the spontaneous polarisation of FLCs with low doping concentration was about twice that of pure FLCs, in addition to a significant improvement in the dielectric properties, the response time and the V-shaped switching in the chiral smectic C (SmC*) phase. The results obtained point the way to an alternative for improving the applicability of FLCs without resorting to chemical synthesis. [ABSTRACT FROM AUTHOR]