Isoda Takeshi, Ushirogochi Hideki, Satoh Koichi, Takasaki Tsuyoshi, Yamamura Itsuki, Sato Chisato, Mihira Ado, Abe Takao, Tamai Satoshi, Yamamoto Shigeki, Kumagai Toshio, Nagao Yoshimitsu
Medical Research Laboratories, Wyeth K.K., 1-6-34 Kashiwa-cho, Shiki-shi, Saitama 353-8511, Japan.
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。
