PMID: 6969724Oct 1, 1980Paper

Mutual pro-drugs of beta-lactam antibiotics and beta-lactamase inhibitors

The Journal of Antibiotics
B BaltzerS Vangedal

Abstract

The principle of combining a beta-lactam antibiotic with a beta-lactamase inhibitor in a single molecule functioning as pro-drug for the two active components is illustrated by the linked esters 3 and 4 in which ampicillin and mecillinam, respectively, are combined with the beta-lactamase inhibitor penicillanic acid sulfone. It is shown that in man these esters are excellently absorbed from the gastro-intestinal tract and after absorption hydrolyzed with simultaneous liberation of the active components. As a result high blood and tissue levels of antibiotic and beta-lactamase inhibitor in a balanced ratio are attained. The advantages of "mutual pro-drugs" over simple combinations are discussed.

Citations

Mar 16, 2019·International Journal of Molecular Sciences·Ana Monserrat-MartinezEmma Sierecki
Apr 3, 2020·Chemical Biology & Drug Design·Sandeep RanaAmarnath Natarajan
Jul 1, 1988·The Journal of Pharmacy and Pharmacology·N M Nielsen, H Bundgaard
Oct 5, 2001·Expert Opinion on Pharmacotherapy·J R Kerr, N W Preston
May 10, 2016·Expert Opinion on Drug Delivery·Ibrahim A AljuffaliJia-You Fang
Apr 28, 2018·Nature Reviews. Drug Discovery·Jarkko RautioMichael J Hageman
Aug 1, 1997·Natural Product Reports·K H BaggaleyC J Schofield
Jun 1, 1989·Antimicrobial Agents and Chemotherapy·R N JonesC Thornsberry

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