Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block

被引：29

作者：

Clark, JK ^{[1
]}

Cowley, P

Muir, AW

Palin, R

Pow, E

Prosser, AB

Taylor, R

Zhang, MQ

机构：

[1] Organon Res Labs Ltd, Dept Med Chem, Newhouse ML1 5SH, Lanark, Scotland

[2] Organon Res Labs Ltd, Dept Pharmacol, Newhouse ML1 5SH, Lanark, Scotland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(02)00482-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series benzylpiperidinium and benzylpyridinium quaternary salts have been synthesised and tested for inhibition of acetylcholinesterase and reversal of neuromuscular block induced by vecuronium. Several potent reversal agents have been identified and their haemodynamic effects measured. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2565 / 2568

页数：4

共 11 条

[1] REVERSAL OF NEUROMUSCULAR BLOCKADE [J].

BEVAN, DR ;

DONATI, F ;

KOPMAN, AF .

ANESTHESIOLOGY, 1992, 77 (04) :785-805

[2]

Brufani Mario, 1997, Drugs of the Future, V22, P397

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

ELLMAN, GL ;

COURTNEY, KD ;

ANDRES, V ;

FEATHERSTONE, RM .

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

[4] Oxyaniliniums as acetylcholinesterase inhibitors for the reversal of neuromuscular block [J].

Grove, SJA ;

Kaur, J ;

Muir, AW ;

Pow, E ;

Tarver, GJ ;

Zhang, MQ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (02) :193-196

[5] The simulated binding of (+/-)-2,3-dihydro-5,6-dimethoxy-2-[[l-(phenylmethyl)-4-piperidinyl]methyl]-1H-inden-1-one hydrochloride (E2020) and related inhibitors to free and acylated acetylcholinesterases and corresponding structure-activity analyses [J].

Inoue, A ;

Kawai, T ;

Wakita, M ;

Iimura, Y ;

Sugimoto, H ;

Kawakami, Y .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (22) :4460-4470

[6] Molecular modelling and QSAR of reversible acetylcholinesterase inhibitors [J].

Kaur, J ;

Zhang, MQ .

CURRENT MEDICINAL CHEMISTRY, 2000, 7 (03) :273-294

[7] The rationale for E2020 as a potent acetylcholinesterase inhibitor [J].

Kawakami, Y ;

Inoue, A ;

Kawai, T ;

Wakita, M ;

Sugimoto, H ;

Hopfinger, AJ .

BIOORGANIC & MEDICINAL CHEMISTRY, 1996, 4 (09) :1429-1446

[8] Novel piperidinium and pyridinium agents as water-soluble acetylcholinesterase inhibitors for the reversal of neuromuscular blockade [J].

Palin, R ;

Clark, JK ;

Cowley, P ;

Muir, AW ;

Pow, E ;

Prosser, AB ;

Taylor, R ;

Zhang, MQ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (18) :2569-2572

[9] SYNTHESIS AND ANTIACETYLCHOLINESTERASE ACTIVITY OF 1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE HYDROCHLORIDE (E2020) AND RELATED-COMPOUNDS [J].

SUGIMOTO, H ;

IIMURA, Y ;

YAMANISHI, Y ;

YAMATSU, K .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1992, 2 (08) :871-876

[10] Donepezil hydrochloride (E2020) and other acetylcholinesterase inhibitors [J].

Sugimoto, H ;

Yamanishi, Y ;

Iimura, Y ;

Kawakami, Y .

CURRENT MEDICINAL CHEMISTRY, 2000, 7 (03) :303-339

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