Literature DB >> 16830892

Syntheses and pharmacokinetic studies of prodrug esters for the development of oral carbapenem, L-084.

Takeshi Isoda1, Hideki Ushirogochi, Koichi Satoh, Tsuyoshi Takasaki, Itsuki Yamamura, Chisato Sato, Ado Mihira, Takao Abe, Satoshi Tamai, Shigeki Yamamoto, Toshio Kumagai, Yoshimitsu Nagao.   

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.

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Year:  2006        PMID: 16830892     DOI: 10.1038/ja.2006.34

Source DB:  PubMed          Journal:  J Antibiot (Tokyo)        ISSN: 0021-8820            Impact factor:   2.649


  4 in total

1.  Synthesis and antibacterial activity of novel lincomycin derivatives. I. Enhancement of antibacterial activities by introduction of substituted azetidines.

Authors:  Ko Kumura; Yoshinari Wakiyama; Kazutaka Ueda; Eijiro Umemura; Takashi Watanabe; Eiki Shitara; Hideki Fushimi; Takuji Yoshida; Keiichi Ajito
Journal:  J Antibiot (Tokyo)       Date:  2016-01-13       Impact factor: 2.649

Review 2.  Carbapenems: past, present, and future.

Authors:  Krisztina M Papp-Wallace; Andrea Endimiani; Magdalena A Taracila; Robert A Bonomo
Journal:  Antimicrob Agents Chemother       Date:  2011-08-22       Impact factor: 5.191

3.  Crystal structures of biapenem and tebipenem complexed with penicillin-binding proteins 2X and 1A from Streptococcus pneumoniae.

Authors:  Mototsugu Yamada; Takashi Watanabe; Nobuyoshi Baba; Yasuo Takeuchi; Fukuichi Ohsawa; Shuichi Gomi
Journal:  Antimicrob Agents Chemother       Date:  2008-04-07       Impact factor: 5.191

4.  Crystal structure of tebipenem pivoxil.

Authors:  Chao Tang; Li Cai; Shuai Liu; Zhiwei Zheng; Gen Li; Jianli Chen; Qiang Sui
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2018-08-10
  4 in total

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