- Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 1
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In an attempt to search for clinically useful antitumor agents, we have discovered that a series of 1,7-disubstituted-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids possessed moderate cytotoxic activity. We investigated the structure-acti
- Tomita, Kyoji,Tsuzuki, Yasunori,Shibamori, Koh-ichiro,Tashima, Masanori,Kajikawa, Fumie,Sato, Yuji,Kashimoto, Shigeki,Chiba, Katsumi,Hino, Katsuhiko
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p. 5564 - 5575
(2007/10/03)
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- Synthesis and Structure-Activity Relationships of New Arylfluoronaphthyridine Antibacterial Agents
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Novel arylfluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid have been prepared and their antibacterial activity evaluated.These derivatives are characterized by having a fluorine atom at 6-position, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position.The in vitro antibacterial potency is greatest when the 1-substituent is either p-fluorophenyl or o,p-difluorophenyl and the 7-substituent is a 3-amino-1-pyrrolidinyl group. 1-(2,4-Difluorophenyl)-6-fluoro-7-(3-amino-1-pyrrolidinyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid (38) was found to possess excellent in vitro potency and in vivo efficacy.
- Chu, Daniel T. W.,Fernandes, Prabhavathi B.,Claiborne, Akiyo K.,Gracey, Eugene H.,Pernet, Andre G.
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p. 2364 - 2369
(2007/10/02)
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