| Title : Synthesis of fluorescent probes directed to the active site gorge of acetylcholinesterase - Saltmarsh_2000_Bioorg.Med.Chem.Lett_10_1523 |
| Author(s) : Saltmarsh JR , Boyd AE , Rodriguez OP , Radic Z , Taylor P , Thompson CM |
| Ref : Bioorganic & Medicinal Chemistry Lett , 10 :1523 , 2000 |
|
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 approximately 10(5) M(-1) min(-1)). Size exclusion chromatography afforded a fluorescently-labeled cholinesterase conjugate. |
| PubMedSearch : Saltmarsh_2000_Bioorg.Med.Chem.Lett_10_1523 |
| PubMedID: 10915041 |
Saltmarsh JR, Boyd AE, Rodriguez OP, Radic Z, Taylor P, Thompson CM (2000)
Synthesis of fluorescent probes directed to the active site gorge of acetylcholinesterase
Bioorganic & Medicinal Chemistry Lett
10 :1523
Saltmarsh JR, Boyd AE, Rodriguez OP, Radic Z, Taylor P, Thompson CM (2000)
Bioorganic & Medicinal Chemistry Lett
10 :1523