45966-19-6Relevant academic research and scientific papers
Novel nonquaternary reactivators showing reactivation efficiency for soman-inhibited human acetylcholinesterase
Wei, Zhao,Liu, Yan-qin,Wang, Yong-an,Li, Wan-hua,Zhou, Xin-bo,Zhao, Jian,Huang, Chun-qian,Li, Xing-zhou,Liu, Jia,Zheng, Zhi-bing,Li, Song
, p. 1 - 6 (2016/02/09)
Soman is a highly toxic nerve agent with strong inhibition of acetylcholinesterase (AChE), but of the few reactivators showing antidotal efficiency for soman-inhibited AChE presently are all permanently charged cationic oximes with poor penetration of the blood-brain barrier. To overcome this problem, uncharged reactivators have been designed and synthesized, but few of them were efficient for treating soman poisoning. Herein, we used a dual site biding strategy to develop more efficient uncharged reactivators. The ortho-hydroxylbenzaldoximes were chosen as reactivation ligands of AChE to prevent the secondary poisoning of AChE, and simple aromatic groups were used as peripheral site ligands of AChE, which were linked to the oximes in a similar way as that found in the reactivator HI-6. The in vitro experiment demonstrated that some of the resulting conjugates have robust activity against soman-inhibited AChE, and oxime 8b was highlighted as the most efficient one. Although not good as HI-6 in vitro, these new compounds hold promise for development of more efficient centrally acting reactivators for soman poisoning due to their novel nonquaternary structures, which are predicted to be able to cross the blood-brain barrier.
SULFONYLAMINO-ACETIC ACID DERIVATIVES
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Page 27, (2010/02/06)
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
REACTIVITY OF NEW PRECURSORS OF QUINONE METHIDES
Loubinoux, Bernard,Miazimbakana, Joseph,Gerardin, Philippe
, p. 1939 - 1942 (2007/10/02)
The azidomethylene protecting group allows the synthesis of unstable phenolic compounds which are used as quinone methide precursors in the alkylations of alcohols, phenols, azide, thiophenol, amines, enols and enolates.
