Author/Authors :
Jennifer R. Saltmarsh، نويسنده , , Aileen E. Boyd، نويسنده , , Oscar P. Rodriguez، نويسنده , , Zoran Radi ، نويسنده , , Palmer Taylor and Jill Trewhella، نويسنده , , Charles M. Thompson، نويسنده ,
Abstract :
Six organophosphorus compounds linked to fluorophore groups were prepared in an effort to selectively modify the active site of acetylcholinesterase and deliver probes to the gorge region. Two compounds that vary by the length of a methylene (CH2) group, pyrene-SO2NH(CH2)nNHC(O)CH2CH2P(O)(OEt)(F) (where n=2 or 3) were found to be potent, irreversible inhibitors of recombinant mouse AChE (Ki 105 M−1 min−1). Size exclusion chromatography afforded a fluorescently-labeled cholinesterase conjugate.
