Synthesis and Molecular Properties of Nerve Agent Reactivator HLö-7 Dimethanesulfonate
| Autor: | S.M. Bester, Scott D. Pegan, J.R. McGuire, Fu-Lian Hsu, J.J. Height, Su Y Bae, Andrew J. Walz, Dana R. Anderson |
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| Rok vydání: | 2019 |
| Předmět: |
010405 organic chemistry
Organic Chemistry Organophosphate Deliberate release Pharmacology Oxime 01 natural sciences Biochemistry Acetylcholinesterase 0104 chemical sciences HLo 7 dimethanesulfonate 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry Drug Discovery medicine Ex vivo Phrenic nerve Nerve agent medicine.drug |
| Zdroj: | ACS Med Chem Lett |
| ISSN: | 1948-5875 |
| DOI: | 10.1021/acsmedchemlett.9b00021 |
| Popis: | [Image: see text] 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. |
| Databáze: | OpenAIRE |
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