|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0007634,
umls-concept:C0020245,
umls-concept:C0086418,
umls-concept:C0205216,
umls-concept:C0205549,
umls-concept:C0220781,
umls-concept:C0279516,
umls-concept:C0332256,
umls-concept:C0441655,
umls-concept:C0596402,
umls-concept:C1533691,
umls-concept:C1883254
|
|
pubmed:issue |
5
|
|
pubmed:dateCreated |
2006-1-27
|
|
pubmed:abstractText |
This report describes 9H-isothiazolo[5,4-b]quinoline-3,4-diones (ITQs) containing aromatic groups at the 7-position that were prepared using palladium-catalyzed cross-coupling and tested against a panel of susceptible and resistant bacteria. In general, these compounds were more effective against Gram-positive than Gram-negative organisms. Many of the ITQs were more potent than contemporary quinolones and displayed a particularly strong antistaphylococcal activity against a clinically important, multi-drug-resistant strain. In contrast with ITQs reported previously, several of the analogues described in this Letter demonstrated low cytotoxic activity against a human cell line.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Mar
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:BradburyBarton JBJ,
pubmed-author:ChengJijunJ,
pubmed-author:DeshpandeMilindM,
pubmed-author:HashimotoAkihiroA,
pubmed-author:LucienEdlaineE,
pubmed-author:MarlorChristopher WCW,
pubmed-author:OuYangsiY,
pubmed-author:PodosSteven DSD,
pubmed-author:PucciMichael JMJ,
pubmed-author:SongYongshengY,
pubmed-author:ThanassiJane AJA,
pubmed-author:ThomaChristy LCL,
pubmed-author:WangQiupingQ,
pubmed-author:WilesJason AJA
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1272-6
|
|
pubmed:meshHeading |
pubmed-meshheading:16337791-Anti-Bacterial Agents,
pubmed-meshheading:16337791-Azo Compounds,
pubmed-meshheading:16337791-Cell Line,
pubmed-meshheading:16337791-Escherichia coli,
pubmed-meshheading:16337791-Humans,
pubmed-meshheading:16337791-Hydrocarbons, Aromatic,
pubmed-meshheading:16337791-Microbial Sensitivity Tests,
pubmed-meshheading:16337791-Molecular Structure,
pubmed-meshheading:16337791-Quinolines,
pubmed-meshheading:16337791-Staphylococcus aureus,
pubmed-meshheading:16337791-Sulfhydryl Compounds
|
|
pubmed:year |
2006
|
|
pubmed:articleTitle |
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
|
|
pubmed:affiliation |
Achillion Pharmaceuticals, Inc., 300 George Street, New Haven, CT 06511-6653, USA. jwiles@achillion.com
|
|
pubmed:publicationType |
Journal Article
|
