New oxime reactivators connected with CH2O(CH2)nOCH2 linker and their reactivation potency for organophosphorus agents-inhibited acetylcholinesterase |
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Authors: | Yang Garp Yeol Oh Kyung-Ae Park No-Joong Jung Young-Sik |
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Institution: | aDrug Discovery Division, Korea Research Institute of Chemical Technology, PO Box 107, Yuseong, Daejeon 305-600, Republic of Korea |
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Abstract: | New bis-pyridinium oxime reactivators 6 with CH2O(CH2)2OCH2 and CH2O(CH2)4OCH2 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 × 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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Keywords: | Organophosphorus agents Bis-pyridinium oxime reactivators Acetylcholinesterase Linker Pesticide |
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