Nucleophilicity of Some Reactivators of Phosphorylated Acetylcholinesterase1

Yacov Ashani; Sasson Cohen; Yacov Ashani; Sasson Cohen

doi:10.1021/jm00289a014

Nucleophilicity of Some Reactivators of Phosphorylated Acetylcholinesterase¹

Yacov Ashani, Sasson Cohen, Yacov Ashani, Sasson Cohen

Physiology Pharmacology

Research output: Contribution to journal › Article › peer-review

Abstract

A rational approach is presented toward the establishment of a structure-activity relationship in a series of reactivators of DFP-inhibited AChE. The value of k_t, the first-order reactivation rate constant, at pH 7.4 is a function of both the nucleophilicity of the reactivator molecule and its basicity, reaching an optimum for compounds with a pK_a value in the range 7.6-8.0.

Original language	English
Pages (from-to)	621-626
Number of pages	6
Journal	Journal of Medicinal Chemistry
Volume	14
Issue number	7
DOIs	https://doi.org/10.1021/jm00289a014
State	Published - 1 Jul 1971

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title = "Nucleophilicity of Some Reactivators of Phosphorylated Acetylcholinesterase1",

abstract = "A rational approach is presented toward the establishment of a structure-activity relationship in a series of reactivators of DFP-inhibited AChE. The value of kt, the first-order reactivation rate constant, at pH 7.4 is a function of both the nucleophilicity of the reactivator molecule and its basicity, reaching an optimum for compounds with a pKa value in the range 7.6-8.0.",

author = "Yacov Ashani and Sasson Cohen and Yacov Ashani and Sasson Cohen",

year = "1971",

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doi = "10.1021/jm00289a014",

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AU - Ashani, Yacov

AU - Cohen, Sasson

AU - Ashani, Yacov

AU - Cohen, Sasson

PY - 1971/7/1

Y1 - 1971/7/1

N2 - A rational approach is presented toward the establishment of a structure-activity relationship in a series of reactivators of DFP-inhibited AChE. The value of kt, the first-order reactivation rate constant, at pH 7.4 is a function of both the nucleophilicity of the reactivator molecule and its basicity, reaching an optimum for compounds with a pKa value in the range 7.6-8.0.

AB - A rational approach is presented toward the establishment of a structure-activity relationship in a series of reactivators of DFP-inhibited AChE. The value of kt, the first-order reactivation rate constant, at pH 7.4 is a function of both the nucleophilicity of the reactivator molecule and its basicity, reaching an optimum for compounds with a pKa value in the range 7.6-8.0.

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M3 - מאמר

AN - SCOPUS:0015088566

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JO - Journal of Medicinal Chemistry

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ER -

Nucleophilicity of Some Reactivators of Phosphorylated Acetylcholinesterase¹

Abstract

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