Document Detail

Phenyl-tetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
MedLine Citation:
PMID:  23148598     Owner:  NLM     Status:  Publisher    
Pyridinium and bis-piridinium aldoximes are used, as antidotes, to reactivate acetylcholinesterase (AChE) inhibited by organophosphorus nerve agents. Herein, we described a series of nine non quaternary phenyl-tetrahydroisoquinoline-pyridinaldoxime conjugates more efficient than, or as efficient as pyridinium oximes to reactivate VX-, tabun- and ethyl paraoxon-inhibited human AChE. This study explores the structure-activity relationships of this new family of reactivators, and show that 1b, 1c and 1d are uncharged hAChE reactivators with a broad spectrum.
Guillaume Mercey; Julien Renou; Tristan Verdelet; Maria Kliachyna; Rachid Baati; Emilie Gillon; Mélanie Arboléas; Mélanie Loiodice; Florian Nachon; Ludovic Jean; Pierre-Yves Renard
Related Documents :
23105108 - Crystal structures of tubulin acetyltransferase reveal a conserved catalytic core and t...
23659468 - Reactive centre loop mutants of α-1-antitrypsin reveal position-specific effects on in...
23224238 - A competitive peptide inhibitor kidari negatively regulates hfr1 by forming nonfunction...
24372098 - Critical domains within the sequence of human organic anion transporting polypeptides.
12697028 - A novel strategy for the development of selective active-site inhibitors of the protein...
16269408 - Deficiency of disulfide bonds facilitating fibrillogenesis of endostatin.
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-14
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  The influence of climatic conditions on the transmission dynamics of the 2009 A/H1N1 influenza pande...
Next Document:  Anopheles salivary gland proteomes from major malaria vectors.