The 3,3'-bis-pyridinium mono-oximes as antidotes against organophosphorous intoxication.
In an attempt to develop effective antidotes against organophosphorous intoxication, three new structurally related bispyridinium mono-oximes with a 2-oxopropane bridge were synthesized. The compounds were evaluated for in-vivo therapeutic protection and cholinesterase reactivation in blood and various brain regions. In neuromuscular function studies against diisopropyl-fluorophosphate and isopropyl methylphosphonofluoridate poisoning, the oximes produced significant protection. The compounds produced marked peripheral reactivation and beneficial effects on neuromuscular transmission. The reactivation of cholinesterase in cerebral cortex by the oximes, in spite of their being quaternary salts is a notable feature.
Sikder
A K
AK
Synthetic Chemistry Division, Defence Research & Development Establishment, Gwalior, India.
Pandey
K S
KS
Jaiswal
D K
DK
Dube
S N
SN
Kumar
D
D
Husain
K
K
Bhattacharya
R
R
Das Gupta
S
S
D000818:Animals; D000931:Antidotes / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D001923:Brain Chemistry; D002802:Cholinesterases / Q000097:blood; D007531:Isoflurophate / Q000633:toxicity*; D008297:Male; D051379:Mice; D009469:Neuromuscular Junction / Q000187:drug effects; D010091:Oximes / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D011726:Pyridinium Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D012524:Sarin / Q000633:toxicity*
D000931:Antidotes; D010091:Oximes; D011726:Pyridinium Compounds; D007531:Isoflurophate; D012524:Sarin; D002802:Cholinesterases