rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
8
|
pubmed:dateCreated |
2006-4-13
|
pubmed:abstractText |
A series of fosmidomycin analogues featuring restricted conformational mobility has been synthesized and evaluated as inhibitors of 1-deoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase and as growth inhibitors of P. falciparum. The enantiomerically pure trans-cyclopropyl N-acetyl analogue 3b showed comparable inhibitory activity as fosmidomycin toward E. coli DOXP reductoisomerase and proved equally active when tested in vitro for P. falciparum growth inhibition. Conversely, the alpha-phenyl cis-cyclopropyl analogue 4 showed virtually no inhibition of the enzyme.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
0022-2623
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
20
|
pubmed:volume |
49
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2656-60
|
pubmed:dateRevised |
2011-11-17
|
pubmed:meshHeading |
pubmed-meshheading:16610809-Aldose-Ketose Isomerases,
pubmed-meshheading:16610809-Animals,
pubmed-meshheading:16610809-Escherichia coli,
pubmed-meshheading:16610809-Fosfomycin,
pubmed-meshheading:16610809-Molecular Structure,
pubmed-meshheading:16610809-Multienzyme Complexes,
pubmed-meshheading:16610809-Oxidoreductases,
pubmed-meshheading:16610809-Parasitic Sensitivity Tests,
pubmed-meshheading:16610809-Plasmodium falciparum,
pubmed-meshheading:16610809-Stereoisomerism,
pubmed-meshheading:16610809-Structure-Activity Relationship
|
pubmed:year |
2006
|
pubmed:articleTitle |
Synthesis and biological evaluation of cyclopropyl analogues of fosmidomycin as potent Plasmodium falciparum growth inhibitors.
|
pubmed:affiliation |
Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.
|
pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|