
Bioorganic and Medicinal Chemistry Letters p. 3107 - 3112 (1997)
Update date:2022-08-05
Topics:
Fan
Paternotte
Vermander
Li
Beaujean
Scorneaux
Dumont
Osinski
Claesen
Tulkens
Sonveaux
Seven new ester prodrugs of ampicillin with hydrolysis half-lives ranging from 65 to 308 min were synthesized. The cellular accumulation of two of them (in J774 mouse macrophages) and their activities against intracellular Staphylococcus aureus were determined in comparison with the pivaloyloxymethylester of ampicillin (pivampicillin) and ampicillin. The esters accumulated extensively and were more active than ampicillin in this in vitro system.
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Doi:10.1016/S0960-894X(97)00390-9
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