用于口服碳青霉烯类药物L-084开发的前药酯的合成及药代动力学研究
Syntheses and pharmacokinetic studies of prodrug esters for the development of oral carbapenem, L-084.
作者信息
Isoda Takeshi, Ushirogochi Hideki, Satoh Koichi, Takasaki Tsuyoshi, Yamamura Itsuki, Sato Chisato, Mihira Ado, Abe Takao, Tamai Satoshi, Yamamoto Shigeki, Kumagai Toshio, Nagao Yoshimitsu
机构信息
Medical Research Laboratories, Wyeth K.K., 1-6-34 Kashiwa-cho, Shiki-shi, Saitama 353-8511, Japan.
出版信息
J Antibiot (Tokyo). 2006 Apr;59(4):241-7. doi: 10.1038/ja.2006.34.
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.
通过对(1R,5S,6S)-6-[(R)-1-羟乙基]-1-甲基-2-[1-(1,3-噻唑啉-2-基)氮杂环丁烷-3-基]硫代-1-碳青霉烯-2-羧酸(LJC11036)的各种前药酯进行药代动力学研究，我们发现了一种口服活性碳青霉烯类药物L-084。L-084对革兰氏阳性菌和革兰氏阴性菌均表现出强大的抗菌活性，并且在LJC11036的合成前药中展现出最高的肠道吸收性。
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