Studies on anti-Helicobacter pylori agents. Part 3: A novel, efficacious cephem derivative, FR193879.

作者信息

Yoshida Yoshiki, Matsuda Keiji, Sasaki Hiroshi, Matsumoto Yoshimi, Matsumoto Satoru, Tawara Shuichi, Takasugi Hisashi

机构信息

Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd, 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan.

出版信息

Bioorg Med Chem Lett. 2004 May 17;14(10):2627-31. doi: 10.1016/j.bmcl.2004.02.068.

DOI:10.1016/j.bmcl.2004.02.068

PMID:15109666

Abstract

The synthesis, therapeutic efficacy against H. pylori, and preliminary safety of the novel cephem derivative, FR193879 (8a) are described. Compound 8a having a (4-carbamoylmethylthiazol-2-yl)thio moiety at the 3-position and a phenylacetamido at the 7-position was found to have good safety showing a nontoxic dose of > 100 mg/kg in dogs in a 4-week repeat dose toxicity study and extremely potent therapeutic efficacy against H. pylori, showing 30 times superior activity compared to AMPC, and did not display cross-resistance with CAM or MNZ.

摘要