[Alkyl sulfates and alkyl aryl sulfonates as inhibitors of penicillinase].
The kinetics of inhibition of penicillinase of Bac. licheniformis 749/c by various alkyl-sulphates (with a long hydrocarbon chain from C8 to C16), n-toluolsulphoacid and alkylbenzol-sulphonate (R-C12--C16) was studied. The inhibition rate increased with elongation of the alkyl radical and rising of the inhibitor concentraiton. This means that the determining factor in inhibition process was hydrophobic interaction of the alkyl chains and not the electrostatic interaction with the enzyme. In-vitro experiments with penicillinase-producing strains of staphylococcus showed that non-bactericidal concentrations of the alkylsulphates and alkylben zolsulphonates increased the effect of benzylpenicillin, ampicillin and methicillin. The highest increase in the antibiotic activity, as well as in the enzyme inhibition was observed with respect to the compound with the hydrocarbon chain fron C12 to C16. The increase in the activity of methicillin against the staphylococcal strains resistant simultaneously to benzylpenicillin, ampicillin and methicillin was indicative of possible using of the above surface active substances as inhibitors of the realization process of various mechanisms of penicillin resistance.
D000476:Alkanesulfonates / Q000494:pharmacology*; D000667:Ampicillin / Q000494:pharmacology; D001190:Arylsulfonates / Q000494:pharmacology*; D001407:Bacillus / Q000201:enzymology; D004791:Enzyme Inhibitors; D007700:Kinetics; D008712:Methicillin / Q000494:pharmacology; D010400:Penicillin G / Q000494:pharmacology; D010403:Penicillin Resistance / Q000187:drug effects; D013210:Staphylococcus / Q000187:drug effects; D013501:Surface-Active Agents; D065093:beta-Lactamase Inhibitors
D000476:Alkanesulfonates; D001190:Arylsulfonates; D004791:Enzyme Inhibitors; D013501:Surface-Active Agents; D065093:beta-Lactamase Inhibitors; D000667:Ampicillin; D010400:Penicillin G; D008712:Methicillin
Alkilsul'faty i alkilarilsul'fonaty kak ingibitory penitsillinazy