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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
25
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pubmed:dateCreated |
1993-1-27
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pubmed:abstractText |
A series of [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acids and their esters were prepared and evaluated for antibacterial activity. The derivatives with a hydrogen or methyl group at C-1, fluorine at C-6, and piperazinyl or 4-methyl-1-piperazinyl group at C-7 showed superior in vitro antibacterial activity, and the derivatives with 4-methyl-1-piperazinyl group at C-7 had potent in vivo activity. Compound 29a (NM394) showed excellent in vitro antibacterial activity and low toxicity but poor absorption from the gastrointestinal tract. Compound 29ee (NM441), an N-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl] derivative of 29a, was found to possess a favorable pharmacokinetic profile and oral activity superior to that of ciprofloxacin in experimental animals.
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pubmed:commentsCorrections | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4727-38
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:1335082-Administration, Oral,
pubmed-meshheading:1335082-Animals,
pubmed-meshheading:1335082-Anti-Infective Agents,
pubmed-meshheading:1335082-Carboxylic Acids,
pubmed-meshheading:1335082-Escherichia coli Infections,
pubmed-meshheading:1335082-Fluoroquinolones,
pubmed-meshheading:1335082-Male,
pubmed-meshheading:1335082-Mice,
pubmed-meshheading:1335082-Microbial Sensitivity Tests,
pubmed-meshheading:1335082-Pseudomonas Infections,
pubmed-meshheading:1335082-Quinolones,
pubmed-meshheading:1335082-Structure-Activity Relationship
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pubmed:year |
1992
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pubmed:articleTitle |
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
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pubmed:affiliation |
Research Laboratories, Nippon Shinyaku Company, Ltd., Kyoto, Japan.
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pubmed:publicationType |
Journal Article
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