Peptidic prodrugs of novel aminomethyl-THF 1β-methylcarbapenems

Yang I. Lin, Panayota Bitha, Subas M. Sakya, Zhong Li, Stanley A. Lang, Youjun Yang, Niraja Bhachech, William J. Weiss, Peter J. Petersen, Nilda V. Jacobus, Karen Bush, Raymond T. Testa

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Abstract

Peptidic prodrugs of the five most active aminomethyl-THF β- methylcarbapenems were synthesized. Of these, only L-amino acid derivatives from la demonstrated an improved oral activity. These results indicate that the L-amino acid derivatives from la are orally absorbed most likely through the dipeptide and tripeptide transport mechanism.

Original languageEnglish
Pages (from-to)1665-1670
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume7
Issue number13
DOIs
StatePublished - 8 Jul 1997

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    Lin, Y. I., Bitha, P., Sakya, S. M., Li, Z., Lang, S. A., Yang, Y., Bhachech, N., Weiss, W. J., Petersen, P. J., Jacobus, N. V., Bush, K., & Testa, R. T. (1997). Peptidic prodrugs of novel aminomethyl-THF 1β-methylcarbapenems. Bioorganic and Medicinal Chemistry Letters, 7(13), 1665-1670. https://doi.org/10.1016/S0960-894X(97)00281-3