Bioorganic and Medicinal Chemistry Letters, volume 9, issue 21, pages 3123-3126

Synthesis and anti-Helicobacter pylori activity of FR182024, a new cephem derivative

Yoshiki YOSHIDA 1
Keiji Matsuda 2
Hiroshi Sasaki 2
Yoshimi Matsumoto 3
Satoru Matsumoto 3
Hisashi Takasugi 2
1
 
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
2
 
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan
3
 
Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan
Publication typeJournal Article
Publication date1999-11-01
scimago Q2
wos Q2
SJR0.508
CiteScore5.7
Impact factor2.5
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
The synthesis and anti-Helicobacter pylori activity of a novel cephem derivative FR182024 (1) are described. FR182024 having a (5-methyl-1,3,4-thiadiazol-2-yl)-thio moiety at the 3-position and a phenylacetamido at the 7-position was found to have extremely potent in vitro anti-H.pylori activity, superior therapeutic efficacy to AMPC and CAM, and low potential for causing diarrhea.

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