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催醒宁(I,R=H,R′X=HCl)对胆碱酯酶的抑制作用较强,但稳定性较差,作用时间较短。推测可能与其酯基易于水解有关。鉴于催醒宁结构中的氨基甲酸酯是抑酶作用的药效基团,酯基被水解后,抑酶活性即消失,我们设想,如果在催醒宁结构中的酯基邻位上引入取代基,利用其空间效应的影响,使酯基增加对水解的稳定性,或有可能达到延长作用时间的目的。因此,我们合成了二甲氨基甲酸-5-(1,3,3-三甲基-6-取代基)吲哚满酯盐酸盐和季铵盐(Ⅰ_(1～14),表1),以探索取代基对抑酶强度和作用时间的影响。
Routine (I, R = H, R’X = HCl) on the inhibition of cholinesterase stronger, but the stability is poor, the action time is shorter. It is speculated that its ester-based hydrolysis may be related. In view of the fact that the carbamate in the arid structure is a pharmacophore that inhibits the action of the enzyme, the depressor activity disappears when the ester group is hydrolyzed, and it is hypothesized that if the ester group ortho to the arid structure is introduced Substituents, the use of their spatial effects, the ester group to increase the stability of the hydrolysis, or may achieve the purpose of prolonging the action time. Therefore, we synthesized indolin-2-yl dimethylcarbamate hydrochloride and quaternary ammonium salts (I_ (1 ~ 14), Table 1) , In order to explore the impact of substituents on the inhibition of the strength and duration of action.