| Title : Synthesis and structure-activity relationships of new acetylcholinesterase inhibitors: Morpholinoalkylcarbamoyloxyeseroline derivatives - Alisi_1995_Bioorg.Med.Chem.Lett_5_2077 |
| Author(s) : Alisi MA , Brufani M , Filocamo L , Gostoli G , Licandro E , Cesta MC , Lappa S , Marchesini D , Pagella P |
| Ref : Bioorganic & Medicinal Chemistry Lett , 5 :2077 , 1995 |
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Abstract :
Several new potent acetylcholinesterase inhibitors have been synthesised as potential drugs for the meatment of Alzheimer's disease. Heptylphysostigmine (MF201) is a drug analogue of physostigmine under clinical evaluation. In order to obtain new physostigmine analogues, the metliylcarbamoyloxy group was substituted with co-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 heptylphysostigmin. |
| PubMedSearch : Alisi_1995_Bioorg.Med.Chem.Lett_5_2077 |
| PubMedID: |
Alisi MA, Brufani M, Filocamo L, Gostoli G, Licandro E, Cesta MC, Lappa S, Marchesini D, Pagella P (1995)
Synthesis and structure-activity relationships of new acetylcholinesterase inhibitors: Morpholinoalkylcarbamoyloxyeseroline derivatives
Bioorganic & Medicinal Chemistry Lett
5 :2077
Alisi MA, Brufani M, Filocamo L, Gostoli G, Licandro E, Cesta MC, Lappa S, Marchesini D, Pagella P (1995)
Bioorganic & Medicinal Chemistry Lett
5 :2077