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Synthesis and Molecular Properties of Nerve Agent Reactivator HLo-7 Dimethanesulfonate.

ABSTRACT: The threat of a deliberate release of chemical nerve agents has underscored the need to continually improve field effective treatments for these types of poisonings. The oxime containing HLö-7 is a potential second-generation therapeutic reactivator. A synthetic process for HLö-7 is detailed with improvements to the DIBAL reduction and ion exchange steps. HLö-7 was visualized for the first time within the active site of human acetylcholinesterase and its relative ex vivo potency confirmed against various nerve agents using a phrenic nerve hemidiaphragm assay.

SUBMITTER: Hsu FL

PROVIDER: S-EPMC6511945 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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Synthesis and Molecular Properties of Nerve Agent Reactivator HLö-7 Dimethanesulfonate.

Hsu Fu-Lian FL Bae Su Y SY McGuire Jack J Anderson Dana R DR Bester Stephanie M SM Height Jude J JJ Pegan Scott D SD Walz Andrew J AJ

ACS medicinal chemistry letters 20190328 5

The threat of a deliberate release of chemical nerve agents has underscored the need to continually improve field effective treatments for these types of poisonings. The oxime containing HLö-7 is a potential second-generation therapeutic reactivator. A synthetic process for HLö-7 is detailed with improvements to the DIBAL reduction and ion exchange steps. HLö-7 was visualized for the first time within the active site of human acetylcholinesterase and its relative <i>ex vivo</i> potency confirmed ...[more]

PMID: 31097996

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