ChemInform Abstract: PREPARATION AND QUATERNATION OF PYRIDINEALDOXIME ALKYL ETHERS

Hagedorn, Ilse; Guendel, W.-H.; Hoose, J; Jenter, Chr.

doi:10.1002/chin.197641254

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“…However, these compounds were unable to effectively reactivate POX-inhibited AChE. 57 Similarly, vinyl analogues of monoquaternary pyridinaldoximes (33-35; Fig. 6) and a vinyl analogue of compound 3 (36; Fig.…”

Section: Other Reactivators Tested Against Opp Poisoningmentioning

confidence: 99%

Design, evaluation and structure—Activity relationship studies of the AChE reactivators against organophosphorus pesticides

Musílek

Doležal

Gunn‐Moore

et al. 2011

Medicinal Research Reviews

113

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Organophosphate pesticides (OPPs; e.g. chlorpyrifos, diazinon, paraoxon) are a wide and heterogeneous group of organophosphorus compounds. Their biological activity of inhibiting acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) ranks them as life endangering agents. The necessary treatment after OPP exposure involves the use of parasympatolytics (e.g. atropine), oxime reactivators (e.g. obidoxime), and anticonvulsive drugs (e.g. diazepam). Therefore, the reactivators of AChE are essential compounds in the treatment of OPP intoxications. Commercial AChE reactivators (e.g. pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) were originally developed for other members of the organophosphate family, such as nerve agents (e.g. sarin, soman, tabun, VX). Pralidoxime, HI-6, and methoxime were found to be weak reactivators of OPP-inhibited AChE. Obidoxime and trimedoxime showed satisfactory reactivation against various OPPs with minor toxicity issues. During the last two decades, the treatment of OPP exposure has become more widely discussed because of growing agricultural production, industrialization, and harmful social issues (e.g. suicides). In this review is the summarized design, evaluation, and structure-activity relationship studies of recently produced AChE reactivators. Since pralidoxime, over 300 oximes have been produced or tested against OPP poisoning, and several novel compounds show very promising abilities as comparable (or higher) to commercial oximes. Some of these are highlighted for their further testing of OPP exposure and, additionally, the main structure-activity relationship of AChE reactivators against OPP is discussed.

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Section: Other Reactivators Tested Against Opp Poisoningmentioning

confidence: 99%

Design, evaluation and structure—Activity relationship studies of the AChE reactivators against organophosphorus pesticides

Musílek

Doležal

Gunn‐Moore

et al. 2011

Medicinal Research Reviews

113

View full text Add to dashboard Cite

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ChemInform Abstract: PREPARATION AND QUATERNATION OF PYRIDINEALDOXIME ALKYL ETHERS

Abstract: Die Pyridinaldoxime (I) werden in Gegenwart von Natriumäthylat O‐alkyliert und die gebildeten Alkyläther (II) mit Dihalogenalkylen (III) in bisquartäre Salze (IV) übergeführt.

Cited by 1 publication

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Design, evaluation and structure—Activity relationship studies of the AChE reactivators against organophosphorus pesticides

Design, evaluation and structure—Activity relationship studies of the AChE reactivators against organophosphorus pesticides

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