Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors |
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Authors: | Tang Huang Ning Fang-Xian Wei Yong-Biao Huang Shi-Liang Huang Zhi-Shu Chan Albert Sun-Chi Gu Lian-Quan |
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Institution: | School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510080, People's Republic of China. |
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Abstract: | A series of 9-aminoalkanamido-1-azabenzanthrones derviatives (3a-i Ar-NHCO(CH(2))(n)NR(1)R(2)) and their quaternary methiodide salts (4a-g Ar-NHCO(CH(2))(n)N(+)(CH(3))R(1)R(2)I(-)) were designed and synthesized as acetylcholinesterase (AChE) or butyrylcholinesterase (BuChE) inhibitors. The synthetic compounds exhibited high AChE inhibitory activity with IC(50) values in the nanomolar range and high selectivity for AChE over BuChE (45- to 1980-fold). The structure-activity relationships (SARs) were discussed. |
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