189157-32-2Relevant academic research and scientific papers
Effect of varying the 4″-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa
Hiraiwa, Yukiko,Minowa, Nobuto,Usui, Takayuki,Akiyama, Yoshihisa,Maebashi, Kazunori,Ikeda, Daishiro
, p. 6369 - 6372 (2008/03/14)
4″-Deoxy-4″-episubstituted arbekacin derivatives and 4″-epi-5-deoxy-5-episubstituted arbekacin derivatives were designed and synthesized. Arbekacin and 4″-epiarbekacin both displayed the same antibacterial activity against Staphylococcus aureus (including
NOVEL AMINOGLYCOSIDE ANTIBIOTIC EFFECTIVE AGAINST METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS (MRSA)
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Page/Page column 51-52, (2010/11/24)
Disclosed are compounds represented by general formula (I) or pharmacologically acceptable salts or solvates thereof having excellent antimicrobial activity against bacteria causative of severe infections such as pneumonia and septicemia, particularly against MRSA, and also antimicrobial agents comprising these compounds, and pharmaceutical compositions comprising these compounds as an active component.
Synthesis of 2''-oxidized derivatives of 5-deoxy-5-epi-5-fluoro-dibekacin and -arbekacin, and study on structure-chemical shift relationships of urethane(or amide)-type NH protons in synthetic intermediates
Kobayashi, Yoshihiko,Tsuchiya, Tsutomu
, p. 261 - 277 (2007/10/03)
Three 2''-modified dibekacin-analogs have been prepared as potential compounds active against resistant bacteria producing 2''-O-phosphotransferases; one is 5-deoxy-5,2''-diepi-5-fluorodibekacin (9) prepared from a suitably protected 2''-O-triflyl derivative through the 2'',3''-cyclic carbamate, and the others are 2''-oxo derivatives (12 and 22, both as the hydrate) of 5-deoxy-5-epi-5-fluoro-dibekacin and -arbekacin prepared through oxidation at C-2'' of suitably protected derivatives. Relationships between the t-butoxycarbonyl(= Boc)-NH-shifts of per-N-Boc synthetic intermediates and their structures were studied. It was found that the shifts, measured in pyridine-d5 at 80 °C, which spread over a close range (δ 6-7 ppm), are sensitively influenced by nearby and surrounding groups around the BocNH group in respect of electron-withdrawing character, hydrogen bonding (BocNH ... acceptor), and also solvent effects (BocNH ... NC5H5).
