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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
22
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pubmed:dateCreated |
1992-12-1
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pubmed:abstractText |
A series of novel 7-substituted-1-tert-butyl-6-fluoronaphthyridone-3- carboxylic acids has been prepared. These derivatives are characterized by chiral aminopyrrolidine substituents at the 7 position. In this paper we report the full details of the asymmetric synthesis of this series of compounds. Structure-activity relationship studies indicate that the absolute stereochemistry at the asymmetric centers of the pyrrolidine ring is critical for maintaining good activity. Compounds 60 and 61 (3-amino-4-methylpyrrolidine enantiomers) were selected for preclinical evaluation.
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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 |
Oct
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
30
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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 |
4205-13
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:1433222-Animals,
pubmed-meshheading:1433222-Anti-Bacterial Agents,
pubmed-meshheading:1433222-Dogs,
pubmed-meshheading:1433222-Female,
pubmed-meshheading:1433222-Gram-Negative Bacteria,
pubmed-meshheading:1433222-Gram-Positive Bacteria,
pubmed-meshheading:1433222-Mice,
pubmed-meshheading:1433222-Microbial Sensitivity Tests,
pubmed-meshheading:1433222-Naphthyridines,
pubmed-meshheading:1433222-Stereoisomerism,
pubmed-meshheading:1433222-Structure-Activity Relationship
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pubmed:year |
1992
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pubmed:articleTitle |
Fluoronaphthyridines and -quinolones as antibacterial agents. 5. Synthesis and antimicrobial activity of chiral 1-tert-butyl-6-fluoro-7-substituted-naphthyridones.
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pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, Marne-la-Vallée, France.
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pubmed:publicationType |
Journal Article
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