- Syntheses and pharmacokinetic studies of prodrug esters for the development of oral carbapenem, L-084
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We discovered an orally active carbapenem, L-084, through pharmacokinetic studies on various prodrug esters of (1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-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. Japan Antibiotics Research Association.
- Isoda, Takeshi,Ushirogochi, Hideki,Satoh, Koichi,Takasaki, Tsuyoshi,Yamamura, Itsuki,Sato, Chisato,Mihira, Ado,Abe, Takao,Tamai, Satoshi,Yamamoto, Shigeki,Kumagai, Toshio,Nagao, Yoshimitsu
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p. 241 - 247
(2007/10/03)
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- Carbapenem-3-carboxylic acid ester derivatives
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Disclosed are carbapenem-3-carboxylic acid ester derivatives of formula (I), wherein R1 is a hydrogen atom or a lower alkyl group, R2 is an alkyl group which may be substituted by a cycloalkyl group having about 4 to 7 carbon atoms and which may be substituted by a lower alkyl group, or is a cycloalkyl group having 4 to 7 carbon atoms which may be substituted by a lower alkyl group and n is 0 or 1. The compounds are highly absorbable through the digestive tract and are rapidly converted in the body to the active compound, which shows strong antibacterial activity. STR1
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