测定了２９个毒扁豆碱类似物的抑制胆碱酯酶活性，对其结构与抑酶活性强度、抑制时间及毒性之间的关系进行了探讨，结果表明：（１）去掉毒扁豆碱的第二个并吡咯环可保持抑酶活性并降低毒性和延长作用时间．（２）胺甲酰氧侧链氮原子上选用较长碳链烷基亦可保持抑酶活性并降低毒性和延长作用时间．（３）二氢吲哚环１位和３位选择较小的烷基取代基时活性较高． The inhibition of cholinesterase activity by 29 analogues of physostigmine was studied. The relationship between the structure and the activity of inhibition enzyme, the inhibition time and the toxicity was investigated. The results showed that: (1) The two pyrrole rings retain their aprotinin activity and reduce toxicity and prolong the duration of action. (2) carbamoyloxy side chain nitrogen atoms longer alkyl chain can be selected to maintain the activity of inhibiting the enzyme and reduce toxicity and prolongation of action time. (3) Indole ring with higher activity when smaller alkyl substituents are selected at positions 1 and 3 of the indoline ring.