Reversible inhibition of human acetylcholinesterase by methoxypyridinium species

Joseph J. Topczewski; Alexander M. Lodge; Sumana N. Yasapala; Maurice K. Payne; Pedrom M. Keshavarzi; Daniel M. Quinn

doi:10.1016/j.bmcl.2013.09.008

Reversible inhibition of human acetylcholinesterase by methoxypyridinium species

Joseph J. Topczewski
, Alexander M. Lodge
, Sumana N. Yasapala
, Maurice K. Payne
, Pedrom M. Keshavarzi
, Daniel M. Quinn

Chemistry (Twin Cities)

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

8 Scopus citations

Abstract

The irreversible inhibition of acetylcholinesterase (AChE) by organophosphorous chemical warfare agents necessitates that antidotes be administered for effective treatment. Currently no antidote is known that resurrects the phosphyl-AChE complex once aging has occurred. This report characterizes the affinities of over 30 new AChE inhibitors which could act as resurrecting agents for the aged AChE-OP adduct.

Original language	English (US)
Pages (from-to)	5786-5789
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	23
Issue number	21
DOIs	https://doi.org/10.1016/j.bmcl.2013.09.008
State	Published - Nov 1 2013

Bibliographical note

Funding Information:
This work was supported by the CounterACT Program, National Institutes of Health Office of the Director, and the National Institute of Neurological Disorders and Stroke, Grant 5 R21 NS076430. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.

Keywords

2-Methoxypyridinium compounds
Acetylcholinesterase
Reversible inhibition

Publisher link

10.1016/j.bmcl.2013.09.008

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title = "Reversible inhibition of human acetylcholinesterase by methoxypyridinium species",

abstract = "The irreversible inhibition of acetylcholinesterase (AChE) by organophosphorous chemical warfare agents necessitates that antidotes be administered for effective treatment. Currently no antidote is known that resurrects the phosphyl-AChE complex once aging has occurred. This report characterizes the affinities of over 30 new AChE inhibitors which could act as resurrecting agents for the aged AChE-OP adduct.",

keywords = "2-Methoxypyridinium compounds, Acetylcholinesterase, Reversible inhibition",

author = "Topczewski, \{Joseph J.\} and Lodge, \{Alexander M.\} and Yasapala, \{Sumana N.\} and Payne, \{Maurice K.\} and Keshavarzi, \{Pedrom M.\} and Quinn, \{Daniel M.\}",

note = "Funding Information: This work was supported by the CounterACT Program, National Institutes of Health Office of the Director, and the National Institute of Neurological Disorders and Stroke, Grant 5 R21 NS076430. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. ",

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AU - Lodge, Alexander M.

AU - Yasapala, Sumana N.

AU - Payne, Maurice K.

AU - Keshavarzi, Pedrom M.

AU - Quinn, Daniel M.

N1 - Funding Information: This work was supported by the CounterACT Program, National Institutes of Health Office of the Director, and the National Institute of Neurological Disorders and Stroke, Grant 5 R21 NS076430. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.

PY - 2013/11/1

Y1 - 2013/11/1

N2 - The irreversible inhibition of acetylcholinesterase (AChE) by organophosphorous chemical warfare agents necessitates that antidotes be administered for effective treatment. Currently no antidote is known that resurrects the phosphyl-AChE complex once aging has occurred. This report characterizes the affinities of over 30 new AChE inhibitors which could act as resurrecting agents for the aged AChE-OP adduct.

AB - The irreversible inhibition of acetylcholinesterase (AChE) by organophosphorous chemical warfare agents necessitates that antidotes be administered for effective treatment. Currently no antidote is known that resurrects the phosphyl-AChE complex once aging has occurred. This report characterizes the affinities of over 30 new AChE inhibitors which could act as resurrecting agents for the aged AChE-OP adduct.

KW - 2-Methoxypyridinium compounds

KW - Acetylcholinesterase

KW - Reversible inhibition

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M3 - Article

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AN - SCOPUS:84885173434

SN - 0960-894X

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 21

ER -

Reversible inhibition of human acetylcholinesterase by methoxypyridinium species

Abstract

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Keywords

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