Lin Gialih, Tseng Hsin-Chang, Chio Ai-Chi, Tseng Tsao-Ming, Tsai Bo-Yi
Department of Chemistry, National Chung-Hsing University, Taichung, Taiwan.
Bioorg Med Chem Lett. 2005 Feb 15;15(4):951-5. doi: 10.1016/j.bmcl.2004.12.058.
Alkane-1-N-butylcarbamate-n-ols (1-7) and 1,n-alkane-di-N-butylcarbamates (8-14) are potent pseudo-substrate inhibitors of acetylcholinesterase. For inhibitors 1-7, the pre-steady state -logK(s) values and steady state -logK(i), values are linearly correlated with the tether length (N). However, for inhibitors 8-14, correlation of the -logK(s) or -logK(i) values against N deviates from linearity. A discontinuity of the -logK(s) versus N plot, concave downwards, is indicative of a rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by inhibitors 8-14.
1-正丁基氨基甲酸烷酯-n-醇(1-7)和1,n-烷二基二正丁基氨基甲酸酯(8-14)是乙酰胆碱酯酶的强效假底物抑制剂。对于抑制剂1-7,预稳态-logK(s)值和稳态-logK(i)值与连接链长度(N)呈线性相关。然而,对于抑制剂8-14,-logK(s)或-logK(i)值与N的相关性偏离线性。-logK(s)对N的图向下凹的不连续性表明抑制剂8-14对乙酰胆碱酯酶抑制的预稳态中存在速率决定步骤的变化。