6-Acetylmethylenepenicillanic acid (Ro 15-1903), a potent beta-lactamase inhibitor. I. Inhibition of chromosomally and R-factor-mediated beta-lactamases.
6-Acetylmethylenepenicillanic acid (Ro 15-1903) was seen to be a powerful inhibitor of various beta-lactamases. Nearly all of the chromosomally and R-factor-mediated beta-lactamases which were studied were inhibited at much lower concentrations than required with clavulanic acid or sulbactam. Ro 15-1903 protected beta-lactamase-labile penicillins and cephalosporins from hydrolysis. The compound itself was stable against hydrolysis and inhibition of beta-lactamase was irreversible.
D001419:Bacteria / Q000648:ultrastructure*; D002511:Cephalosporins / Q000378:metabolism; D002876:Chromosomes, Bacterial / Q000201:enzymology*; D006868:Hydrolysis; D010397:Penicillanic Acid / Q000494:pharmacology* / Q000031:analogs & derivatives; D010406:Penicillins / Q000378:metabolism; D011815:R Factors / Q000187:drug effects*; D065093:beta-Lactamase Inhibitors
D002511:Cephalosporins; D010406:Penicillins; D065093:beta-Lactamase Inhibitors; C036977:6-acetylmethylenepenicillanic acid; D010397:Penicillanic Acid