| 17869525 |
Yang GY, Oh KA, Park NJ, Jung YS: New oxime reactivators connected with CH2O (CH2) nOCH2 linker and their reactivation potency for organophosphorus agents-inhibited acetylcholinesterase. Bioorg Med Chem. 2007 Dec 15;15(24):7704-10. Epub 2007 Sep 1.
New bis-pyridinium oxime reactivators 6 with CH (2) O (CH (2))(2) OCH (2) and CH (2) O (CH (2))(4) OCH (2) linkers between the two pyridinium rings were designed and synthesized. In the in vitro test of their potency to reactivate AChE inhibited by organophosphorus agents at 5 x 10 (-3) M concentration, the reactivation ability of 1,2-dimethoxy-ethylene-bis-N,N'-4-pyridiumaldoxime dichloride (6a) was 63% for housefly (HF) AChE inhibited by diisopropyl fluorophosphates (DFP), 51% for bovine red blood cell (RBC) AChE inhibited by DFP, 67% for HF-AChE inhibited by paraoxon, and 81% for RBC-AChE inhibited by paraoxon. Except in the case of DFP-inhibited HF AChE test of 2-PAM, the activities of 6a are much higher than the activities of 2-PAM and HI-6 which are AChE reactivators currently in use. |
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