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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1987-4-15
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pubmed:abstractText |
A series of pyridobenzothiazine acid derivatives was synthesized and their in vitro antibacterial activity was evaluated. The 1,4-benzothiazine intermediates, which by Gould-Jacobs quinoline synthesis produced pyridobenzothiazine acids, were prepared by hydrolytic basic cleavage of substituted 2-aminobenzothiazoles and successive cyclocondensation with 1-bromo-2-chloroethane or alternatively with monochloroacetic acid, hence reduction by LiAlH4. The pyridobenzothiazine acids 10c, 30, and 31 show potent antibacterial activities against Gram-positive and Gram-negative pathogens. Structure-activity relationships are discussed. The compound 9-fluoro-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-d e] [1,4]benzothiazine-6-carboxylic acid (31) (MF-934) has been found to possess, together with the antibacterial activity, a weak acute toxicity and interesting pharmacokinetic characteristics in several animal species (rat, dog, monkey, man).
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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 |
Mar
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
465-73
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3820216-Anti-Bacterial Agents,
pubmed-meshheading:3820216-Chromatography, High Pressure Liquid,
pubmed-meshheading:3820216-Gram-Negative Bacteria,
pubmed-meshheading:3820216-Gram-Positive Bacteria,
pubmed-meshheading:3820216-Indicators and Reagents,
pubmed-meshheading:3820216-Magnetic Resonance Spectroscopy,
pubmed-meshheading:3820216-Microbial Sensitivity Tests,
pubmed-meshheading:3820216-Pyridones,
pubmed-meshheading:3820216-Spectrophotometry, Infrared,
pubmed-meshheading:3820216-Thiazines
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pubmed:year |
1987
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pubmed:articleTitle |
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
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pubmed:publicationType |
Journal Article,
Comparative Study
|