- Syntheses and pharmacokinetic studies of prodrug esters for the development of oral carbapenem, L-084.
Syntheses and pharmacokinetic studies of prodrug esters for the development of oral carbapenem, L-084.
The Journal of antibiotics (2006-07-13)
Takeshi Isoda, Hideki Ushirogochi, Koichi Satoh, Tsuyoshi Takasaki, Itsuki Yamamura, Chisato Sato, Ado Mihira, Takao Abe, Satoshi Tamai, Shigeki Yamamoto, Toshio Kumagai, Yoshimitsu Nagao
PMID16830892
ABSTRACT
We discovered an orally active carbapenem, L-084, through pharmacokinetic studies on various prodrug esters of (1R,5S,6S)-6-[(R)-1-hydroxyethyl]-l-methyl-2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-1-carbapen-2-em-3-carboxylic acid (LJC11,036). L-084 showed a strong antimicrobial activity against Gram-positive and Gram-negative bacteria and exhibited the highest intestinal absorption among synthesized prodrugs of LJC11,036.
MATERIALI