Abstract
In order to design orally active carbapenem antibiotics effective against β-lactam-resistant pathogens, such as penicillin-resistant Streptococcus pneumoniae (PRSP) and β-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 β-lactams.
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Sunagawa, M., Ueda, Y., Okada, Si. et al. Orally Active Carbapenem Antibiotics I. J Antibiot 58, 787–803 (2005). https://doi.org/10.1038/ja.2005.106
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DOI: https://doi.org/10.1038/ja.2005.106