[Relation of the structure, rate of hydrolysis and activity of dicarboxylic acid esters].
The kinetics of enzymatic cholinesterase hydrolysis of dicarboxylic acid esters with neuromuscular blocking activity was studied in vitro. The maximum hydrolysis rate was shown to increase on elongation of the distance between ester groups both in the compounds containing a hydrophobic adamantyl radical attached to quaternary nitrogen and in bis-esters not containing adamantyl radicals. The comparison of neuromuscular blocking activity in vivo, enzymatic hydrolysis rates and activity on isolated skeletal muscle of some compounds demonstrated that in vivo activity is in a higher correlation with the maximum hydrolysis rate of the compounds that with activity in isolated skeletal muscle before or after cholinesterase inhibition.
Kharkevich
D A
DA
Skoldinov
A P
AP
Lemina
E Iu
EIu
Igumnova
N D
ND
D000009:Abdominal Muscles / Q000187:drug effects / Q000201:enzymology; D000818:Animals; D002802:Cholinesterases / Q000378:metabolism; D003998:Dicarboxylic Acids / Q000493:pharmacokinetics / Q000494:pharmacology*; D006736:Horses; D006868:Hydrolysis; D066298:In Vitro Techniques; D009388:Neostigmine / Q000494:pharmacology; D003473:Neuromuscular Nondepolarizing Agents; D011898:Ranidae; D013329:Structure-Activity Relationship
D003998:Dicarboxylic Acids; D003473:Neuromuscular Nondepolarizing Agents; D009388:Neostigmine; D002802:Cholinesterases
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