4-Aminopyridine derivatives with antiamnesic activity

作者: A Andreani

DOI: 10.1016/S0223-5234(00)00103-3

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摘要: Acetylcholine (Ach) enhancement, useful in the treatment of Alzheimer's disease (AD), may be obtained by means ion channel modulators such as 4-aminopyridine (4-AP). 4-AP is also central ring tacrine, first drug approved for AD. The synthesis and pharmacological activity three derivatives, prepared with aim improving their antiamnesic activity, here described. In two these compounds connected to 4-aminobutyric acid (GABA), whereas third it 2-indolinone, i.e., skeleton linopirdine, another Ach enhancing agent. new showed potent comparison piracetam.

参考文章(15)
Michael Davidson, Zvi Zemishlany, Richard C. Mohs, Thomas B. Horvath, Peter Powchik, John P. Blass, Kenneth L. Davis, 4-Aminopyridine in the treatment of alzheimer's disease Biological Psychiatry. ,vol. 23, pp. 485- 490 ,(1988) , 10.1016/0006-3223(88)90020-0
G. Van Eys, H. Rigter, B.E. Leonard, Time-dependent aspects of CO2 induced amnesia and hippocampal monoamine metabolism in rats Pharmacology Biochemistry and Behavior. ,vol. 3, pp. 787- 793 ,(1975) , 10.1016/0091-3057(75)90108-2
A. Lenègre, R. Chermat, I. Avril, L. Stéru, R.D. Porsolt, Specificity of piracetam's anti-amnesic activity in three models of amnesia in the mouse. Pharmacology, Biochemistry and Behavior. ,vol. 29, pp. 625- 629 ,(1988) , 10.1016/0091-3057(88)90030-5
E. M. Hawes, D. K. J. Gorecki, 2-amino-3-substituted 1,6-naphthyridines Journal of Heterocyclic Chemistry. ,vol. 9, pp. 703- 706 ,(1972) , 10.1002/JHET.5570090338
E. C. TAYLOR, ALDO J. CROVETTI, PYRIDINE-1-OXIDES. I. SYNTHESIS OF SOME NICOTINIC ACID DERIVATIVES1 Journal of Organic Chemistry. ,vol. 19, pp. 1633- 1640 ,(1954) , 10.1021/JO01375A012
Troels Staehelin Jensen, Bent De Fine Olivarius, Transient global amnesia as a manifestation of transient cerebral ischemia Acta Neurologica Scandinavica. ,vol. 61, pp. 115- 124 ,(2009) , 10.1111/J.1600-0404.1980.TB01473.X
S. Thesleff, Aminopyridines and synaptic transmission Neuroscience. ,vol. 5, pp. 1413- 1419 ,(1980) , 10.1016/0306-4522(80)90002-0
F Wilcoxon, J T Litchfield, A SIMPLIFIED METHOD OF EVALUATING DOSE-EFFECT EXPERIMENTS Journal of Pharmacology and Experimental Therapeutics. ,vol. 96, pp. 99- 113 ,(1949)
S W Tam, A R Logue, C M Maciag, J A Saydoff, W J Tinker, R Zaczek, Studies on the role of K+, Cl- and Na+ ion permeabilities in the acetylcholine release enhancing effects of linopirdine (DuP 996) in rat cortical slices. Journal of Pharmacology and Experimental Therapeutics. ,vol. 271, pp. 891- 897 ,(1994)