rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
3
|
pubmed:dateCreated |
2005-1-24
|
pubmed:abstractText |
Systematic SAR studies on the HTS hit pyridine-2-carboxylic acid thiazol-2-ylamide (PACT) analogues revealed that the scaffold of PCAT is indispensable for the inhibition of type I MetAP. For effective inhibition of the enzyme, the most suitable position to modify is the 3-position of the pyridine ring of PCAT, and the best substituents are those containing O or N atoms connected directly with the pyridine ring. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Feb
|
pubmed:issn |
0960-894X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
15
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
635-8
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:15664828-Amides,
pubmed-meshheading:15664828-Aminopeptidases,
pubmed-meshheading:15664828-Anti-Bacterial Agents,
pubmed-meshheading:15664828-Antifungal Agents,
pubmed-meshheading:15664828-Bacterial Proteins,
pubmed-meshheading:15664828-Escherichia coli,
pubmed-meshheading:15664828-Humans,
pubmed-meshheading:15664828-Inhibitory Concentration 50,
pubmed-meshheading:15664828-Pyridines,
pubmed-meshheading:15664828-Salmonella typhimurium,
pubmed-meshheading:15664828-Structure-Activity Relationship,
pubmed-meshheading:15664828-Thiazoles,
pubmed-meshheading:15664828-Thioamides
|
pubmed:year |
2005
|
pubmed:articleTitle |
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold.
|
pubmed:affiliation |
Chinese National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 189 Guoshoujing Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China.
|
pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
|