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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2007-1-15
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pubmed:abstractText |
A novel series of 3-morpholino rifamycins in which the C25 acetate group was replaced by a carbamate group were prepared and found to exhibit significantly improved antimicrobial activity than rifampin against Mycobacterium smegmatis. Further characterization of such compounds suggests that relatively large groups attached to the rifamycin core via a C25 carbamate linkage prevent inactivation via ribosylation of the C23 alcohol as catalyzed by the endogenous rifampin ADP-ribosyl transferase of M. smegmatis. SAR studies of the C25 carbamate rifamycin series against M. smegmatis and other bacteria are reported.
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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 |
Jan
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BonventreEricE,
pubmed-author:ChapoKatrinaK,
pubmed-author:CombrinkKeith DKD,
pubmed-author:DentonDaniel ADA,
pubmed-author:DoyleTimothy BTB,
pubmed-author:HarranSusanS,
pubmed-author:LynchAnthony SAS,
pubmed-author:MaZhenkunZ,
pubmed-author:RobertsonGregory TGT,
pubmed-author:RocheEric DED,
pubmed-author:YanDalaiD
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
522-6
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pubmed:meshHeading |
pubmed-meshheading:17070048-ADP Ribose Transferases,
pubmed-meshheading:17070048-Anti-Bacterial Agents,
pubmed-meshheading:17070048-Drug Resistance, Bacterial,
pubmed-meshheading:17070048-Escherichia coli,
pubmed-meshheading:17070048-Magnetic Resonance Spectroscopy,
pubmed-meshheading:17070048-Microbial Sensitivity Tests,
pubmed-meshheading:17070048-Mycobacterium smegmatis,
pubmed-meshheading:17070048-Pseudomonas aeruginosa,
pubmed-meshheading:17070048-Rifampin,
pubmed-meshheading:17070048-Rifamycins,
pubmed-meshheading:17070048-Staphylococcus aureus,
pubmed-meshheading:17070048-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
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pubmed:affiliation |
Department of Chemistry, Cumbre Pharmaceuticals Inc., 1502 Viceroy Drive, Dallas, TX 75235, USA. kcombrink@cumbrepharma.com
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pubmed:publicationType |
Journal Article
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