Literature DB >> 17847708

Synthesis of a novel series of non-symmetrical bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.

Kamil Musilek1, Ondrej Holas, Kamil Kuca, Daniel Jun, Vlastimil Dohnal, Martin Dolezal.   

Abstract

Nine potential non-symmetrical xylene-bridged AChE reactivators were synthesized using modifications of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and the insecticide paraoxon together with nine symmetrical xylene-bridged compounds, was tested in vitro. Seven compounds were promising against paraoxon-inhibited AChE. Two compounds were found to be more potent against tabun-inhibited AChE than obidoxime at a concentration applicable in vivo.

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Year:  2007        PMID: 17847708     DOI: 10.1080/14756360601164960

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  6 in total

1.  Revealing the importance of linkers in K-series oxime reactivators for tabun-inhibited AChE using quantum chemical, docking and SMD studies.

Authors:  Shibaji Ghosh; Nellore Bhanu Chandar; Kalyanashis Jana; Bishwajit Ganguly
Journal:  J Comput Aided Mol Des       Date:  2017-06-23       Impact factor: 3.686

2.  Bisquaternary pyridinium oximes: Comparison of in vitro reactivation potency of compounds bearing aliphatic linkers and heteroaromatic linkers for paraoxon-inhibited electric eel and recombinant human acetylcholinesterase.

Authors:  Sandip B Bharate; Lilu Guo; Tony E Reeves; Douglas M Cerasoli; Charles M Thompson
Journal:  Bioorg Med Chem       Date:  2009-11-27       Impact factor: 3.641

3.  New series of monoquaternary pyridinium oximes: Synthesis and reactivation potency for paraoxon-inhibited electric eel and recombinant human acetylcholinesterase.

Authors:  Sandip B Bharate; Lilu Guo; Tony E Reeves; Douglas M Cerasoli; Charles M Thompson
Journal:  Bioorg Med Chem Lett       Date:  2009-07-10       Impact factor: 2.823

4.  Efficacy of eight experimental bispyridinium oximes against paraoxon-induced mortality: comparison with the conventional oximes pralidoxime and obidoxime.

Authors:  S M Nurulain; D E Lorke; M Y Hasan; M Shafiullah; K Kuca; K Musilek; G A Petroianu
Journal:  Neurotox Res       Date:  2009-04-07       Impact factor: 3.911

Review 5.  The Experimental Oxime K027-A Promising Protector From Organophosphate Pesticide Poisoning. A Review Comparing K027, K048, Pralidoxime, and Obidoxime.

Authors:  Dietrich E Lorke; Georg A Petroianu
Journal:  Front Neurosci       Date:  2019-05-22       Impact factor: 4.677

6.  Broad-Spectrum Antidote Discovery by Untangling the Reactivation Mechanism of Nerve-Agent-Inhibited Acetylcholinesterase.

Authors:  Cecilia Lindgren; Nina Forsgren; Norman Hoster; Christine Akfur; Elisabet Artursson; Lotta Edvinsson; Richard Svensson; Franz Worek; Fredrik Ekström; Anna Linusson
Journal:  Chemistry       Date:  2022-06-07       Impact factor: 5.020

  6 in total

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