Igumnova N D, Lemina E Iu, Bitiukova I I, Klimova N V, Skoldinov A P
Farmakol Toksikol. 1988 Nov-Dec;51(6):38-41.
The kinetics of cholinesterase enzymatic hydrolysis of carboxylic acid adamantyl derivatives was studied in vitro. The maximal rate of enzymatic hydrolysis in the series of bis-esters was shown to increase on elongation of the distance between ester groups. The maximal hydrolysis rate in the series of bis- and mono-esters decreases on elongation of the distance between ester group and quaternary nitrogen atom. The addition of adamantyl radical to the alcohol part of the molecule of bis- and mono-esters prevents the hydrolysis. The addition of lipophilic radicals to the cationic group of derivatives of mono- and dicarboxylic acids exerts a greater effect on the maximal hydrolysis rate in monoesters than in bis-esters.
在体外研究了羧酸金刚烷基衍生物的胆碱酯酶酶促水解动力学。结果表明，在双酯系列中，酶促水解的最大速率随着酯基之间距离的延长而增加。在双酯和单酯系列中，最大水解速率随着酯基与季氮原子之间距离的延长而降低。在双酯和单酯分子的醇部分添加金刚烷基可防止水解。在单羧酸和二羧酸衍生物的阳离子基团上添加亲脂性基团，对单酯最大水解速率的影响比对双酯的影响更大。
