Fluorinated phosphorus compounds Part 4. A lack of anticholinesterase activity for four tris(fluoroalkyl) phosphates

Citation
Cm. Timperley et al., Fluorinated phosphorus compounds Part 4. A lack of anticholinesterase activity for four tris(fluoroalkyl) phosphates, J FLUORINE, 107(1), 2001, pp. 155-158
Citations number
14
Categorie Soggetti
Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF FLUORINE CHEMISTRY
ISSN journal
00221139 → ACNP
Volume
107
Issue
1
Year of publication
2001
Pages
155 - 158
Database
ISI
SICI code
0022-1139(200101)107:1<155:FPCP4A>2.0.ZU;2-Z
Abstract
Whilst examining the chemistry of a series of tris(fluoroalkyl) phosphates as potential fire retardants. concern was raised over their possible antich olinesterase activity. Bimolecular rate constants (k(t) values) for the inh ibition of bovine erythrocyte acetylcholinesterase (AChE) at 37 degreesC an d pH 7.4 were therefore sought for four fluoroalkyl phosphates: (CF3CH2O)(3 )P=O, (C2F5CH2O)(3)P=O, (C3F7CH7O)(3)P=O and (CF3CH2O)(2)P(O)OCH2C2F5. Unde r the experimental conditions used, none of them inhibited AChE; it was onl y possible to define their ki values as being less than 7-16 M-1 min(-1). T hey are therefore at least a factor of 10(5) less potent inhibitors than th e nerve agents sarin or soman, and should be non-toxic via the mechanism of direct inhibition of AChE. (C) 2001 Elsevier Science B.V. All rights reser ved.