Ester prodrugs of ampicillin tailored for intracellular accumulation

被引：10

作者：

Fan, HJ

Paternotte, I

Vermander, M

Li, K

Beaujean, M

Scorneaux, B

Dumont, P

Osinski, P

Claesen, M

Tulkens, PM

Sonveaux, E

机构：

[1] Univ Catholique Louvain, Ecole Pharm, Unite Chim Pharmaceut & Radiopharm, B-1200 Brussels, Belgium

[2] Univ Catholique Louvain, Ecole Pharm, Unite Pharmacol Cellulaire & Mol, B-1200 Brussels, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(97)10146-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 1997 Elsevier Science Ltd.

引用

页码：3107 / 3112

页数：6

共 25 条

[1]

ALEXANDER JW, 1968, J LAB CLIN MED, V71, P971

[2]

BAKKERWOUDENBERG IAJM, 1989, J PHARMACOL EXP THER, V251, P321

[3]

BARBER HJ, 1953, J APPL CHEM, V3, P253

[4] COUPLING PRODUCTS OF AMINO-ACIDS TO PENICILLIN-V AND CEPHALOTHIN - SYNTHESIS AND SUSCEPTIBILITY TO CARBOXYPEPTIDASES AND LYSOSOMAL-ENZYMES [J].