Syntheses and Pharmacokinetic Studies of Prodrug Esters for the Development of Oral Carbapenem, L-084

We discovered an orally active carbapenem, L-084, through pharmacokinetic studies on various prodrug esters of (1 R ,5 S ,6 S )-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 ag...

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Veröffentlicht in:	Journal of antibiotics 2006-04, Vol.59 (4), p.241-247
Hauptverfasser:	Isoda, Takeshi, Ushirogochi, Hideki, Satoh, Koichi, Takasaki, Tsuyoshi, Yamamura, Itsuki, Sato, Chisato, Mihira, Ado, Abe, Takao, Tamai, Satoshi, Yamamoto, Shigeki, Kumagai, Toshio, Nagao, Yoshimitsu
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Anti-Bacterial Agents - administration & dosage Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacokinetics Anti-Bacterial Agents - pharmacology Bacteria Bacteriology Biological Availability Biomedical and Life Sciences Bioorganic Chemistry Carbapenems - administration & dosage Carbapenems - chemical synthesis Carbapenems - pharmacokinetics Carbapenems - pharmacology Carboxylic acids Esters Gram-Negative Bacteria - drug effects Gram-Positive Bacteria - drug effects Humans Life Sciences Medicinal Chemistry Microbiology Molecular Structure Organic Chemistry original-article Pharmacokinetics Prodrugs - administration & dosage Prodrugs - chemical synthesis Prodrugs - pharmacokinetics Prodrugs - pharmacology Rats
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Zusammenfassung:	We discovered an orally active carbapenem, L-084, through pharmacokinetic studies on various prodrug esters of (1 R ,5 S ,6 S )-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.
ISSN:	0021-8820 1881-1469
DOI:	10.1038/ja.2006.34