Relationship between acute toxicity and in vitro inhibition and hydrolysis of a series of carbalkoxy homologs of malathion

摘要: A series of carbalkoxy homologs malathion and malaoxon was prepared in which the dicarbalkoxy groups were varied from methyl to butyl. The acute oral toxicities these compounds determined using male Wistar rats, it found that decreased with an increase chain length. Inhibiting carboxylesterase vivo tri-o-tolyl phosphate (TOCP) demonstrated both substrates for carboxylesterase, important detoxication malaoxon. In vitro studies rat liver as showed Km values length, whereas Vmax increased findings indicated had greatest hydrolytic activity toward carb-n-butoxy group followed by n-propyl, ethyl, isopropyl, homologs. inhibition bimolecular rate constant decrease length erythrocyte cholinesterase a reverse trend serum cholinesterase. toxicity correlate enzymatic patterns.