Synthesis and Molecular Properties of Nerve Agent Reactivator HLö‑7 Dimethanesulfonate

Synthesis and Molecular Properties of Nerve Agent Reactivator HLö‑7 Dimethanesulfonate

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...

Full description

Saved in:
Bibliographic Details
Published in:ACS medicinal chemistry letters Vol. 10; no. 5; pp. 761 - 766
Main Authors: Hsu, Fu-Lian, Bae, Su Y, McGuire, Jack, Anderson, Dana R, Bester, Stephanie M, Height, Jude J, Pegan, Scott D, Walz, Andrew J
Format: Journal Article
Language:English
Published: United States American Chemical Society 09-05-2019
American Chemical Society (ACS)
Subjects:
Letter
organophosphate
VX
reactivator
nerve agent
7
Acetylcholinesterase
HLö
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
Bibliography:DOE - OTHER
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.9b00021