Potent acetylcholinesterase inhibitors: Design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts

Bioorganic and Medicinal Chemistry Letters

Volumn 10, Issue 7, 2000, Pages 637-639

  Guillou, Catherine ^a   Mary, Aude ^a   Renko, Dolor Zafiarisoa ^a   Gras, Emmanuel ^a   Thal, Claude ^a  

^a INSTITUT DE CHIMIE DES SUBSTANCES NATURELLES   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINESTERASE; CHOLINESTERASE INHIBITOR; GALANTAMINE; TACRINE;

ARTICLE; CHEMICAL MODIFICATION; DRUG DESIGN; DRUG INHIBITION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ELECTROPHORUS; ENZYME INHIBITION; NONHUMAN; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ACETYLCHOLINESTERASE; CHOLINESTERASE INHIBITORS; DIMERIZATION; DRUG DESIGN; GALANTAMINE; STRUCTURE-ACTIVITY RELATIONSHIP;

ELECTROPHORUS; STAPHYLOCOCCUS PHAGE 3A;

EID: 0034599814     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(00)00059-7     Document Type: Article

References (19)

1. (a) Perry, E. K. Br. Med. Bull. 1986, 42, 63.
2. (b) Bartus, R. T.; Dean, L. D.; Beer, B.; Lippa, A. S.; Science 1982, 217, 408.
3. (a) Harvey, A. L. Pharmac. Ther. 1995 68, 113.
4. (b) Mucke, H. A. M. Drugs of Today 1997, 33, 251.
5. (c) Kewitz, H. Drugs of Today 1997, 33, 265.
6. (d) Rainer, M. Drugs of Today 1997, 33, 273
7. (a) Sweeney, T.; Kewitz, H. Life Sciences 1990 46, 1553.
8. (b) Thomsen, T.; Bickel, U.; Fischer, J. P.; Kewitz, H. Eur. J. Clin. Pharmacol. 1990, 39, 603.
9. Han, S. Y.; Sweeney, J. E.; Bachman, E. S.; Schweiger, E. J.; Forloni, G.; Coyle, J. T.; Davis, B. M.; Joullié, M. M. Eur. J. Med. Chem. 1992, 27, 673.
10. Bores, G. M.; Kosley, R. W., Jr. Drugs of the Future 1996, 21, 621.
11. (a) Novel galanthamine derivatives. Thai, C.; Guillou, C.; Mary, A.; Renko, D. Z.; Potier, P.; Christen, Y. PCT Int. Appl. WO 97 03, 987, 19 July 1996, GB Appl.95/14821.9, 19 July 1995.
12. (b) Mary, A.; Renko, D. Z.; Guillou, C.; Thai, C. Bioorg. Med. Chem. 1998, 6 1835.
13. Sussman, J. L.; Harel, M.; Frolow, F.; Oefner, C.; Goldman, A.; Toker, L.; Silman, I. Science 1991, 253, 872.
14. Harel, M.; Schalk, I.; Ehret-Sabatier, L.; Bouet, F.; Goeldner, M.; Hirth, C.; Axelsen, P. H.; Silman, I.; Sussman, J. L. Proc. Natl. Acad. Sci. USA 1993, 90, 9031.
15. (a) Pang, Y. P.; Quiram, P.; Jelacic, T.; Hong, F.; Brimijoin, S. J. Biol. Chem. 1996, 271, 23646.
16. (b) Pang, Y. P.; Hong, F.; Quiram, P.; Jelacic, T.; Brimijoin, S. J. Chem. Soc. Perkin Trans. 1 1997, 171.
17. Carlier, P. R.; Du, D. M.; Han, Y.; Liu, J.; Pang, Y. P. Bioorg. Med. Chem. Lett. 1999, 9, 2335.
18. Mary, A.; Renko, D. Z.; Guillou, C.; Thai, C. Tetrahedron Lett. 1997, 38, 5151.
19. Ellman, G. L.; Courtney, K. D.; Andres, V.; Featherstone, R. M. Biochem. Pharmacol. 1961, 7, 88.