Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
Bioorg Med Chem Lett
; 17(11): 3172-6, 2007 Jun 01.
Article
en En
| MEDLINE
| ID: mdl-17383875
Six novel AChE reactivators with a (Z)-but-2-ene linker were synthesized using the known synthetic pathways. Their ability to reactivate AChE, which had been previously inhibited by nerve agent tabun or pesticide paraoxon, was tested in vitro and compared to pralidoxime, HI-6, obidoxime, and K075. The novel synthesized compounds were found to be ineffective against GA-inhibited AChE but the ability of (Z)-1,4-bis(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide to reactivate paraoxon-inhibited AChE was comparable with that of oxime K075. Notably, the oxime group in position four substantially increased the ability of the novel compounds to reactivate paraoxon-inhibited AChE.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Oximas
/
Paraoxon
/
Organofosfatos
/
Compuestos de Piridinio
/
Inhibidores de la Colinesterasa
/
Reactivadores de la Colinesterasa
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
República Checa
Pais de publicación:
Reino Unido