74704-03-3Relevant academic research and scientific papers
studies on anti-helicobacter pylori agents. Part 2: New cephem derivatives
Yoshida, Yoshiki,Matsuda, Keiji,Sasaki, Hiroshi,Matsumoto, Yoshimi,Matsumoto, Satoru,Tawara, Shuichi,Takasugi, Hisashi
, p. 2317 - 2335 (2007/10/03)
The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of cephem derivatives are described. Introduction of thio-heterocyclic groups containing N- and S-atoms to the 3-position and phenyl or thienyl acetamido groups to the 7-position of the cephem nucleus dramatically improved the activity. From this series of derivatives, compound 13i was found to have extremely potent in vitro anti-H. pylori activity, superior therapeutic efficacy compared to AMPC and CAM, no cross-resistance between CAM or MNZ and low potential for causing diarrhea due to instability to β-lactamase. Copyright (C) 2000 Elsevier Science Ltd.
Orally active cephalosporins. Part 2: Synthesis, structure-activity relationships and oral absorption of cephalosporins having a C-3 pyridyl side chain
Yamamoto, Hirofumi,Terasawa, Takeshi,Nakamura, Ayako,Kawabata, Kohji,Sakane, Kazuo,Matsumoto, Satoru,Matsumoto, Yoshimi,Tawara, Shuichi
, p. 1159 - 1170 (2007/10/03)
A series of 7β-[(Z)-2-(2-aminothiazol-4-yl)-2- hydroxyiminoacetamido]cephalosporins having a pyridine ring connected through various spacer moieties at the C-3 position was designed and synthesized and evaluated for antibacterial activity and oral absorption in rats. All compounds showed potent antibacterial activity against Staphylococcus aureus, whereas antibacterial activity against Gram-negative bacteria was markedly influenced by the spacer moiety between the pyridine and cephem nucleus. Oral absorption was influenced by the position of the pyridine nitrogen as well as by the spacer moiety. Among these compounds, FR86830 (14), having a 4- pyridylmethylthio moiety at the C-3 position, showed the most well balanced activity and moderate oral absorption. (C) 2000 Elsevier Science Ltd.
