Esterase profile of O-phosphorylated ethyltrifluorolactates in prediction of their therapeutic and toxic effects.

作者信息

Rudakova E V, Makhaeva G F, Galenko T G, Aksinenko A Yu, Sokolov V B, Richardson R J, Martynov I V

机构信息

Institute of Physiologically Active Compounds, Russian Academy of Sciences, Severny pr. 1, Chernogolovka, Moscow oblast, 142432 Russia.

出版信息

Dokl Biochem Biophys. 2012 Mar-Apr;443:81-5. doi: 10.1134/S1607672912020068. Epub 2012 May 5.

DOI:10.1134/S1607672912020068

PMID:22562631

Abstract

摘要

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Esterase profile of O-phosphorylated ethyltrifluorolactates in prediction of their therapeutic and toxic effects.

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Synthesis of organophosphates with fluorine-containing leaving groups as serine esterase inhibitors with potential for Alzheimer disease therapeutics.含氟离去基团的有机磷酸酯作为丝氨酸酯酶抑制剂的合成及其在阿尔茨海默病治疗中的潜力。

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5528-30. doi: 10.1016/j.bmcl.2009.08.065. Epub 2009 Aug 21.

Dokl Biochem Biophys. 2008 Nov-Dec;423:352-7. doi: 10.1134/s1607672908060094.

Selective butyrylcholinesterase inhibition elevates brain acetylcholine, augments learning and lowers Alzheimer beta-amyloid peptide in rodent.选择性丁酰胆碱酯酶抑制可提高啮齿动物大脑中的乙酰胆碱水平，增强学习能力并降低β-淀粉样肽。

Proc Natl Acad Sci U S A. 2005 Nov 22;102(47):17213-8. doi: 10.1073/pnas.0508575102. Epub 2005 Nov 7.

Cholinesterase inhibitors: new roles and therapeutic alternatives.胆碱酯酶抑制剂：新作用及治疗选择

Pharmacol Res. 2004 Oct;50(4):433-40. doi: 10.1016/j.phrs.2003.11.017.

Quantitative structure-activity relationships predict the delayed neurotoxicity potential of a series of O-alkyl-O-methylchloroformimino phenylphosphonates.定量构效关系预测了一系列O-烷基-O-甲基氯亚氨基苯基膦酸酯的迟发性神经毒性潜力。

J Toxicol Environ Health A. 2003 Apr 11;66(7):611-25. doi: 10.1080/15287390309353770.

A stable preparation of hen brain neuropathy target esterase for rapid biochemical assessment of neurotoxic potential of organophosphates.

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Comparative studies of O,O-dialkyl-O-chloromethylchloroformimino phosphates: interaction with neuropathy target esterase and acetylcholinesterase.O,O-二烷基-O-氯甲基氯代甲亚胺基磷酸酯的比较研究：与神经病变靶酯酶和乙酰胆碱酯酶的相互作用

Neurotoxicology. 1998 Aug-Oct;19(4-5):623-8.

[Interaction of dialkyl(alpha-carbomethoxy-beta,beta,beta-trifluoro- ethyl) phosphates with mammalian esterases].

Bioorg Khim. 1987 Jan;13(1):33-7.

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