Synthesis and anti-Helicobacter pylori activity of FR182024, a new cephem derivative.
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.
Yoshida
Y
Y
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Matsuda
K
K
Sasaki
H
H
Matsumoto
Y
Y
Matsumoto
S
S
Takasugi
H
H
D000658:Amoxicillin / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology; D017291:Clarithromycin / Q000494:pharmacology; D004195:Disease Models, Animal; D016480:Helicobacter pylori / Q000187:drug effects*; D007769:Lactams; D051379:Mice; D015394:Molecular Structure; D001618:beta-Lactamases / Q000378:metabolism; D047090:beta-Lactams / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D007769:Lactams; D047090:beta-Lactams; D000658:Amoxicillin; C400931:FR 182024; D001618:beta-Lactamases; D017291:Clarithromycin