Orally active carbapenem antibiotics I. Antibacterial and pharmacokinetic potential of 2-phenyl and 2-thienylcarbapenems.
J Antibiot (Tokyo)
; 58(12): 787-803, 2005 Dec.
Article
en En
| MEDLINE
| ID: mdl-16506696
ABSTRACT
In order to design orally active carbapenem antibiotics effective against beta-lactam-resistant pathogens, such as penicillin-resistant Streptococcus pneumoniae (PRSP) and beta-lactamase non-producing ampicillin-resistant Haemophilus influenzae (BLNAR), a series of novel 2-phenylcarbapenems and some 2-thienyl derivatives were synthesized and tested for antibacterial activities. These compounds were highly active against PRSP, BLNAR, and major Gram-positive and Gram-negative bacteria that cause community-acquired infections. Their pivaloyloxymethylester-type prodrug exhibited good oral absorption in mice, suggesting that this series of carbapenems were promising as a prototype of novel orally active beta-lactams.
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Banco de datos:
MEDLINE
Asunto principal:
Tiofenos
/
Carbapenémicos
/
Antibacterianos
Límite:
Animals
/
Humans
/
Male
Idioma:
En
Año:
2005
Tipo del documento:
Article