[Mechanism of the "acetylene effect" during interaction of organophosphorus compounds with cholinesterases].
Here we present data on the anticholinesterase activity of 58 synthesized ethers of phosphorus thioacids with an acetylene bond in the thioether group. Anticholinesterase activity of the compounds, with acetylene group in beta and especially alpha position, in the thioether radical is many times that of their saturated analogs. Reaction between the enzymes and acetylene organophosphorous inhibitors, as well as their saturated analogs, results in phosphorylated enzyme. The triple bond plays a significant role in the acceleration of cholinesterases phosphorylation. Antienzyme activity of acetylene organophosphorous inhibitors is discussed.
Kabachnik
M I
MI
Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Moscow, Russia.
Godovikov
N N
NN
Vikhreva
L A
LA
Pudova
T A
TA
Brestkin
A P
AP
Rozengart
V I
VI
D000110:Acetylcholinesterase / Q000737:chemistry*; D000114:Acetylene / Q000031:analogs & derivatives* / Q000737:chemistry*; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000737:chemistry*; D006736:Horses; D006793:Houseflies; D006801:Humans; D006868:Hydrolysis; D066298:In Vitro Techniques; D007313:Insecta; D007700:Kinetics; D051379:Mice; D008925:Mites; D009943:Organophosphorus Compounds / Q000737:chemistry*; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D009943:Organophosphorus Compounds; D000110:Acetylcholinesterase; D000114:Acetylene
O mekhanizme "atsetilenovogo éffecta" pri vzaimodeĭstvii fosfororganicheskikh soedineniĭ s kholinésterazami.