Influence of the conformation of amide analogs of acetylcholine on their cholinomimetic activity

NV Khromov-Borisov, LN Aleksandrova…

文献索引：Khromov-Borisov, N. V.; Aleksandrova, L. N.; Danilov, A. F.; Shelkovnikov, S. A. Pharmaceutical Chemistry Journal, 1984 , vol. 18, # 6 p. 401 - 403 Khimiko-Farmatsevticheskii Zhurnal, 1984 , vol. 18, # 6 p. 689 - 691

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摘要

According to the data of theorstical conformational analysis, in the amide Ilb a trans- conformation of the fragment N--C--C--N predominates, while in the amide IIIb this fragment is practically fixed in a gauche conformation. On the basis of the results obtained we hypothesized that in the interaction of I and its amide analogs II~ and IIIb with nicstine cholinoreceptors, the gauche-conformation of the fragments OC--C--N (in I) and N--C--C--N (in IIb and IIIb) is active. Continuing ...