Volume 50, Issue 2 pp. 417-424
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Synthesis and Antibacterial Activity of 3-(Substituted arylmethyl)-4-acylaminomethyloxazolidin-2-ones and Derivatization to Symmetrical Twin-Drug Type Molecules

Fumiko Fujisaki

Fumiko Fujisaki

Faculty of Pharmaceutical Sciences, Fukuoka University, Nanakuma, Jonan-ku, Fukuoka, 814-0180 Japan

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Sachi Hiromatsu

Sachi Hiromatsu

Faculty of Pharmaceutical Sciences, Fukuoka University, Nanakuma, Jonan-ku, Fukuoka, 814-0180 Japan

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Yumiko Matsumura

Yumiko Matsumura

Faculty of Pharmaceutical Sciences, Fukuoka University, Nanakuma, Jonan-ku, Fukuoka, 814-0180 Japan

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Aki Fukami

Aki Fukami

Faculty of Pharmaceutical Sciences, Fukuoka University, Nanakuma, Jonan-ku, Fukuoka, 814-0180 Japan

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Nobuhiro Kashige

Nobuhiro Kashige

Faculty of Pharmaceutical Sciences, Fukuoka University, Nanakuma, Jonan-ku, Fukuoka, 814-0180 Japan

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Fumio Miake

Fumio Miake

Faculty of Pharmaceutical Sciences, Fukuoka University, Nanakuma, Jonan-ku, Fukuoka, 814-0180 Japan

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Kunihiro Sumoto

Corresponding Author

Kunihiro Sumoto

Faculty of Pharmaceutical Sciences, Fukuoka University, Nanakuma, Jonan-ku, Fukuoka, 814-0180 Japan

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First published: 03 April 2013
Citations: 6

Abstract

In connection with our studies on antibacterial active compounds in the class of new oxazolidinones against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) strains, some molecular modifications were attempted. In this study, molecular modifications of 4-aminomethyloxazolidin-2-ones (3a) to the corresponding 4-acylaminomethyloxazolidin-2-one derivatives (3c–d) and preparations of the represented twin-drug type molecules (10–14) were investigated. Some additional 4-dialkylaminomethyloxazolidin-2-ones (2) were also synthesized. The synthesized compounds were evaluated for antibacterial activity with Gram-positive (S. aureus) and Gram-negative (E. coli) strains.

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