Acetylcholinesterase inhibition by tacrine analogues

被引：35

作者：

Valenti, P ^{[1
]}

Rampa, A ^{[1
]}

Bisi, A ^{[1
]}

Andrisano, V ^{[1
]}

Cavrini, V ^{[1
]}

Fin, L ^{[1
]}

Buriani, A ^{[1
]}

Giusti, P ^{[1
]}

机构：

[1] UNIV PADUA,DEPT PHARMACOL,I-35131 PADUA,ITALY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(97)10025-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Analogues of tacrine were synthesized and evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity. Compound 2a was the most potent inhibitor of AChE with a higher selectivity than tacrine for AChE over BuChE. Tacrine, on the other hard, showed the opposite behaviour with a weaker inhibitory effect on AChE than on BuChe. The compounds displayed correlated activities in isolated enzymes as well as in rat brain homogenates. (C) 1997 Elsevier Science Ltd.

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页码：2599 / 2602

页数：4

相关论文

共 20 条

[1] The nature of the inhibition of camel retina acetylcholinesterase (EC 3.1.1.7) activity by tetrahydroaminoacridine [J].

AlJafari, AA .

JOURNAL OF OCULAR PHARMACOLOGY AND THERAPEUTICS, 1996, 12 (04) :503-514

[2] The direct introduction of the amino group into aromatic and heterocyclic nuclei V The action of metallic amides on the phenyl and benzoquinolines [J].

Bergstrom, FW .

JOURNAL OF ORGANIC CHEMISTRY, 1938, 3 (05) :424-433

[3]

BERMAN HA, 1992, MOL PHARMACOL, V41, P412

[4] ANTICHOLINESTERASE ACTIVITY OF A NEW CARBAMATE, HEPTYLPHYSOSTIGMINE, IN VIEW OF ITS USE IN PATIENTS WITH ALZHEIMER-TYPE DEMENTIA [J].

BRUFANI, M ;

MARTA, M ;

POMPONI, M .

EUROPEAN JOURNAL OF BIOCHEMISTRY, 1986, 157 (01) :115-120

[5] SYNTHESES, RESOLUTION, AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF POTENT ACETYLCHOLINESTERASE INHIBITORS - 8-CARBAPHYSOSTIGMINE ANALOGS [J].

CHEN, YPL ;

NIELSEN, J ;

HEDBERG, K ;

DUNAISKIS, A ;

JONES, S ;

RUSSO, L ;

JOHNSON, J ;

IVES, J ;

LISTON, D .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (08) :1429-1434

[6]

EAGGER SA, 1991, LANCET, V337, P889

[7] A NEW AND RAPID COLORIMETRIC DETERMINATION OF ACETYLCHOLINESTERASE ACTIVITY [J].

ELLMAN, GL ;

COURTNEY, KD ;

ANDRES, V ;

FEATHERSTONE, RM .

BIOCHEMICAL PHARMACOLOGY, 1961, 7 (02) :88-&

[8] DETERMINATION OF GLUTATHIONE IN PHARMACEUTICALS AND COSMETICS BY HPLC WITH UV AND FLUORESCENCE DETECTION [J].

GOTTI, R ;

ANDRISANO, V ;

CAVRINI, V ;

BONGINI, A .

CHROMATOGRAPHIA, 1994, 39 (1-2) :23-28

[9] CHEMICAL AND PHARMACOLOGICAL CHARACTERIZATION OF GALANTHAMINE, AN ACETYLCHOLINESTERASE INHIBITOR, AND ITS DERIVATIVES - A POTENTIAL APPLICATION IN ALZHEIMERS-DISEASE [J].

HAN, SY ;

SWEENEY, JE ;

BACHMAN, ES ;

SCHWEIGER, EJ ;

FORLONI, G ;

COYLE, JT ;

DAVIS, BM ;

JOULLIE, MM .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1992, 27 (07) :673-687

[10]

HAREL M, 1993, P NATL ACAD SCI USA, V90, P4173