Synthesis and Anticholinesterase Properties of Choline esters of α-Amino Acids

被引：2

作者：

Topuzyan, V. O. ^{[1
]}

Karapetyan, I. R. ^{[1
]}

Alebyan, G. P. ^{[2
]}

机构：

[1] Natl Acad Sci Republ Armenia, Sci Technol Ctr Organ & Pharmaceut Chem, Yerevan, Armenia

[2] Sci Res Inst Biotechnol, Yerevan, Armenia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2014年 / 48卷 / 03期

关键词：

amino acids; choline esters; anticholinesterase properties; HUMAN BUTYRYLCHOLINESTERASE; ACETYLCHOLINESTERASE; REAGENT;

D O I：

10.1007/s11094-014-1070-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-(Dimethylamino)ethyl esters of a number of N-substituted alpha-amino acids and their quaternary ammonium salts were synthesized and their physiochemical properties were determined. We report here studies of their interactions with erythrocyte acetylcholinesterase and human plasma butyrylcholinesterase. IC50 values (the concentrations of study compounds producing 50% inhibition of the rate of cholinesterase hydrolysis of 0.1 mM acetylcholine) were measured for all the compounds synthesized. The results showed that all the choline esters of N-substituted amino acids synthesized here had anticholinesterase properties, mainly specific for butyrylcholinesterase.

引用

页码：163 / 165

页数：3

共 11 条

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

ELLMAN, GL ;

COURTNEY, KD ;

ANDRES, V ;

FEATHERSTONE, RM .

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

[2] ELECTROPHORETIC ANALYSIS OF MAJOR POLYPEPTIDES OF HUMAN ERYTHROCYTE MEMBRANE [J].

FAIRBANKS, G ;

STECK, TL ;

WALLACH, DFH .

BIOCHEMISTRY, 1971, 10 (13) :2606-+

[3]

Giacobini E., 2003, BUTYRYLCHOLINESTERAS

[4]

Grigoryan A. A., 2006, Khimiko-Farmatsevticheskii Zhurnal, V40, P18

[5]

Grigoryan A. A., 2005, BIOTEKHNOL, P59

[6] α,β-dehydrophenylalanine choline esters, a new class of reversible inhibitors of human acetylcholinesterase and butyrylcholinesterase [J].

Grigoryan, Hasmik A. ;

Hambardzumyan, Artur A. ;

Mkrtchyan, Marina V. ;

Topuzyan, Vigen O. ;

Halebyan, Ghukas P. ;

Asatryan, Ruben S. .

CHEMICO-BIOLOGICAL INTERACTIONS, 2008, 171 (01) :108-116

[7] PHENOTYPIC AND MOLECULAR BIOLOGICAL ANALYSIS OF HUMAN BUTYRYLCHOLINESTERASE VARIANTS [J].

LADU, BN ;

BARTELS, CF ;

NOGUEIRA, CP ;

HAJRA, A ;

LIGHTSTONE, H ;

VANDERSPEK, A ;

LOCKRIDGE, O .

CLINICAL BIOCHEMISTRY, 1990, 23 (05) :423-431

[8] ELLMANS REAGENT - 5,5'-DITHIOBIS(2-NITROBENZOIC ACID) - RE-EXAMINATION [J].

RIDDLES, PW ;

BLAKELEY, RL ;

ZERNER, B .

ANALYTICAL BIOCHEMISTRY, 1979, 94 (01) :75-81

[9]

Topuzyan V. O., 1997, Khimiko-Farmatsevticheskii Zhurnal, V31, P25

[10]

TOPUZYAN VO, 1991, ZH ORG KHIM+, V27, P2418

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