SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NEW ACETYLCHOLINESTERASE INHIBITORS - MORPHOLINOALKYLCARBAMOYLOXYESEROLINE DERIVATIVES

被引：17

作者：

ALISI, MA

BRUFANI, M

FILOCAMO, L

GOSTOLI, G

LICANDRO, E

CESTA, MC

LAPPA, S

MARCHESINI, D

PAGELLA, P

机构：

[1] UNIV ROMA LA SAPIENZA,DIPARTIMENTO SCI BIOCHIM A ROSSI FANELLI,I-00185 ROME,ITALY

[2] UNIV MILAN,DIPARTIMENTO CHIM ORGAN & IND,I-20133 MILAN,ITALY

[3] MEDIOLANUM FARMACEUT SPA,I-20143 MILAN,ITALY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 18期

关键词：

D O I：

10.1016/0960-894X(95)00371-Y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several new potent acetylcholinesterase inhibitors have been synthesised as potential drugs for the treatment of Alzheimer's disease. Heptylphysostigmine (MF201) is a drug analogue of physostigmine under clinical evaluation. In order to obtain new physostigmine analogues, the methylcarbamoyloxy group was substituted with omega-morpholinoalkylcarbamoyloxy moieties of different chain lengths (C2-C12). Potent in vitro inhibition is seen when the chain length is composed of eight to twelve methylene groups. The inhibitory activity of the C10 and C11 is 7-fold greater with respect to heptylphysostigmine.

引用

页码：2077 / 2080

页数：4

共 14 条

[1]

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