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The prototype 2 and target compounds 4a-b were prepared from 9-chloro-1,2,3,4-tetrahydro-acridine(7a-c) and α,ω-diamine under microwave irradiation,respectively.Compared with the conventional method,this method is simple,rapid and efficient.On the other hand,Four novel acetylcholinesterase inhibitors,triazole-linked tacrine-based homodimers,were synthesized from N-(8-Chloro-1,2,3,4-tetrahydro-acridin-9-yl)-N-prop-2-ynylhexane- 1,6-diamine,N-(8-Chloro-1,2,3,4-tetrahydro-acridin-9-yl)-N-prop-2-ynyl-heptane-1,7-diamine and (2-azido- ethyl)-(6-chloro-1,2,3,4-tetrahydro-acridin-9-yl)-amine by microwave-assisted Huisgen[3+2] cycloaddition reaction.The structures of novel tacrine-based homodimers were determined by 1H NMR,13C NMR and HRMS.The preliminary bioassay showed that all of them exhibited better AChE (electrophorus) inhibitory activity (Table 1).Particularly,the IC50 values of compounds 6a and 6b were 1.26 and 0.5pM respectively,which were 2.61×105 and 6.58×105 times respectively more potent than tacrine(IC50=329nM,electrophorus).Moreover,as can be seen (Table 1),the 1.5-triazoles-linked tacrine dimers(6a-b) showed much better AChE inhibitory activity than the alkylene-linked tacrine dimmers(2,4a and 4b),but the 1.4-triazoles-linked tacrine dimmers(5a-b) were lower than 2,4a and 4b.So we considered that the triazoles were not only passive linkers,but also active pharmacophores that might contribute significantly to protein binding.The results provided a foundation for future design and development of dual binding site AChE inhibitors.