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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2008-4-24
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pubmed:abstractText |
The design and synthesis of 16-membered macrolides modified at the C-3 position are described. Starting from fully protected intermediate (5), appropriate modifications including Heck reaction were performed to furnish 3-O-(3-aryl-2-propenyl)leucomycin A(7) analogues (9a-9m). These leucomycin A(7) derivatives showed improved in vitro antibacterial activities against clinically important pathogens including erythromycin-resistant Streptococcus pneumoniae (ERSP). SAR analysis of derivatives modified at the C-3 and C-3'' positions suggested that single modification at C-3 or C-3'' was effective for in vitro antibacterial activity.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3391
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4401-18
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pubmed:meshHeading |
pubmed-meshheading:18329276-Anti-Bacterial Agents,
pubmed-meshheading:18329276-Benzoquinones,
pubmed-meshheading:18329276-Crystallography, X-Ray,
pubmed-meshheading:18329276-Drug Design,
pubmed-meshheading:18329276-Kitasamycin,
pubmed-meshheading:18329276-Miocamycin,
pubmed-meshheading:18329276-Models, Molecular,
pubmed-meshheading:18329276-Molecular Structure,
pubmed-meshheading:18329276-Streptococcus,
pubmed-meshheading:18329276-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Design and synthesis of novel leucomycin analogues modified at the C-3 position. Part II: 3-O-(3-Aryl-2-propenyl)leucomycin analogues.
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pubmed:affiliation |
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama 222-8567, Japan. takeshi_furuuchi@meiji.co.jp
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pubmed:publicationType |
Journal Article
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