1. Synthesis and anticholinesterase activity of some new fluorogenic analogues of organophosphorus nerve agents
- Author
-
Christopher M. Timperley, David J. Sellers, Stuart Notman, Krystal E. Casey, Gareth R. Williams, Nancy E. Williams, and Nichola H. Williams
- Subjects
Sarin ,Trifluoromethyl ,Stereochemistry ,Organic Chemistry ,Russian-VX ,Cyclosarin ,General Medicine ,Biochemistry ,Acetylcholinesterase ,Inorganic Chemistry ,chemistry.chemical_compound ,chemistry ,Soman ,medicine ,Environmental Chemistry ,Physical and Theoretical Chemistry ,Tabun ,Nerve agent ,medicine.drug - Abstract
Eighteen new fluorogenic analogues of organophosphorus nerve agents were synthesised and characterised. They included analogues of tabun, sarin, cyclosarin, soman, VX, and Russian VX, with the 7-oxy-4-methylcoumarin or 7-oxy-4-(trifluoromethyl)coumarin leaving group. These analogues inhibited acetylcholinesterase (AChE) effectively in vitro and therefore have potential as tools for the identification of novel organophosphatases in biological systems. Analogues of VX and Russian VX with the 7-amino-4-methylcoumarin group, although poor AChE inhibitors, may have utility for screening enzyme libraries for phosphoramidases capable of cleaving PāN bonds.
- Published
- 2006