Synthesis and anticholinesterase activity of some new fluorogenic analogues of organophosphorus nerve agents
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 P-N bonds.
Timperley, Christopher M.,Casey, Krystal E.,Notman, Stuart,Sellers, David J.,Williams, Nancy E.,Williams, Nichola H.,Williams, Gareth R.
p. 1554 - 1563
(2008/09/18)
Synthesis of new O,O -dialkyl-O-coumarinophosphorothioates and their pesticidal bioassay against Helicoverpa armigera
A series of compounds O,O-dialkyl-O-coumarinophosphorothioates have been synthesized and screened for pesticidal activities against Helicoverpa armigera. Some of the compounds (3,4,6 and 7) show significant activities while rest of the compounds show moderate activities.
Chavan, Vishal P.,Mane, Avinash S.,Shingare, Murlidhar S.
p. 339 - 341
(2007/10/03)
Synthesis of (diethyl-d10) coumaphos and related compounds
Two deuterated insecticides were prepared for use as internal standards for gas-liquid chromatographic-mass spectrometric analyses. Diethyl chlorothiophosphate-d10 was prepared by reaction of ethanol-d6 with P2S5 to give labeled diethyldithiophosphoric acid, followed by chlorination. Treatment of the acid chloride with 3-chloro-4-methyl-7-hydroxycoumarin and potassium carbonate in acetone at reflux gave labeled coumaphos. An analogous reaction with 4-methyl-7-hydroxycoumarin gave labeled potasan, and the technique should be usable for synthesis of labeled forms of other dialkyl thiophosphate insecticides.
Kochansky, Jan
p. 2826 - 2828
(2007/10/03)
Condensation products
Formamidine compounds of the formula EQU1 or WHEREIN R1 represents a substituted or unsubstituted phenyl radical, R2 represents hydroogen, alkyl, alkenyl or alkinyl and R3 represents acyl their manufacture and their use in pest control.