[Phosphorus-containing inhibitors of penicillin acylase. 4. Irreversible inhibition of penicillin acylase from Escherichia coli by monoaryl esters of benzylphosphonic acid].
Monoaryl of benzylphosphonic acid have been synthesized and studied as the inhibitors of penicillin acylase. These compounds were found to be effective and selective irreversible inhibitors of the enzyme. The kinetic parameters of enzyme inactivation are determined, and possible mechanism of the inhibition is discussed. These phosphonates should be useful as both penicillin acylase active site titrants and the tools for the enzyme function study. Benzylchloromethyl keton has been also prepared and it is an irreversible inhibitor of penicillin acylase.
Solodenko
V A
VA
Tserniuk
V N
VN
Shishkina
I P
IP
Galushko
S V
SV
Kukhar'
V P
VP
D001593:Benzyl Compounds / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000201:enzymology*; D004952:Esters; D006843:Hydrocarbons, Chlorinated / Q000494:pharmacology; D007700:Kinetics; D015394:Molecular Structure; D063065:Organophosphonates / Q000494:pharmacology*; D010399:Penicillin Amidase / Q000037:antagonists & inhibitors*; D010758:Phosphorus / Q000032:analysis*; D013329:Structure-Activity Relationship
D001593:Benzyl Compounds; D004791:Enzyme Inhibitors; D004952:Esters; D006843:Hydrocarbons, Chlorinated; D063065:Organophosphonates; D010758:Phosphorus; D010399:Penicillin Amidase