In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker.
A series of bis-pyridinium oximes connected by xylene linker were synthesized and their in-vitro reactivation potential was evaluated against acetylcholinesterase (AChE) inhibited by nerve agent, sarin. Among the synthesized compounds, alpha,alpha'xylene-bis-[3,3'-(hydroxyiminomethyl) pyridinium] dibromide (3b) was found to be most potent reactivator for AChE inhibited by sarin. The oxime 3b exhibits 34% regeneration of inhibited AChE, in comparison to 20 and 15% regeneration by 2-PAM and obidoxime, respectively, at a concentration of 10(-4) M within 10 min.
Acharya
Jyotiranjan
J
Process Technology Development Division, Defence Research & Development Establishment, Jhansi Road, Gwalior, Madhya Pradesh 474002, India. jracharya@rediffmail.com
Gupta
Arvind Kumar
AK
Mazumder
Avik
A
Dubey
Devendra Kumar
DK
D000818:Animals; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004593:Electrophorus; D066298:In Vitro Techniques; D010091:Oximes / Q000737:chemistry / Q000494:pharmacology*; D011726:Pyridinium Compounds / Q000737:chemistry / Q000494:pharmacology*; D012524:Sarin / Q000494:pharmacology*; D014992:Xylenes / Q000737:chemistry*
D002800:Cholinesterase Inhibitors; D010091:Oximes; D011726:Pyridinium Compounds; D014992:Xylenes; D012524:Sarin