Source:http://linkedlifedata.com/resource/pubmed/id/21277200
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2011-2-21
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pubmed:abstractText |
We have designed and synthesized econazole-derived nitroimidazoles to investigate the antitubercular activity of the nitroimidazole compounds. The introduction of a nitro group at the 4-position of the imidazole on econazole abolished the antitubercular activity. However, alcoholic nitroimidazoles 4 and 6 compounds were active against Mycobacterium tuberculosis (Mtb). While the MIC value of econazole was 16 ?g/mL, the MIC of 6a and 6f turned out to be 0.5 ?g/mL. In particular, the activity of 6f against non-replicating Mtb was as good as PA-824, which is currently in clinical phase II studies as an antitubercular agent. Overall, alcohol compounds 4 and 6 tend to be more active than ether compounds 5 and 7.
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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 |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1515-8
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pubmed:meshHeading |
pubmed-meshheading:21277200-Antifungal Agents,
pubmed-meshheading:21277200-Antitubercular Agents,
pubmed-meshheading:21277200-Cyclization,
pubmed-meshheading:21277200-Drug Design,
pubmed-meshheading:21277200-Econazole,
pubmed-meshheading:21277200-Microbial Sensitivity Tests,
pubmed-meshheading:21277200-Molecular Structure,
pubmed-meshheading:21277200-Nitroimidazoles
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pubmed:year |
2011
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pubmed:articleTitle |
Synthesis and antitubercular activity of monocyclic nitroimidazoles: insights from econazole.
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pubmed:affiliation |
Cancer & Infectious Diseases Research Center, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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