|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
22
|
|
pubmed:dateCreated |
2004-10-14
|
|
pubmed:abstractText |
A new class of the HCV NS5b RNA-dependent RNA polymerase inhibitors, the dihyroxypyrimidinecarboxylic acid derivative, was designed from a diketoacid and meconic acid derivative discovered by screening. Mechanism of action and essential moieties required for activity were identified. The corresponding N-methylpyrimidinone was also prepared; both classes are novel, reversible, and selective inhibitors of the HCV NS5b polymerase with improved druglike characteristics.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Oct
|
|
pubmed:issn |
0022-2623
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
21
|
|
pubmed:volume |
47
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
5336-9
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:15481971-Animals,
pubmed-meshheading:15481971-Binding Sites,
pubmed-meshheading:15481971-Drug Design,
pubmed-meshheading:15481971-Hepacivirus,
pubmed-meshheading:15481971-Isomerism,
pubmed-meshheading:15481971-Keto Acids,
pubmed-meshheading:15481971-Microsomes, Liver,
pubmed-meshheading:15481971-Models, Molecular,
pubmed-meshheading:15481971-Pyrimidines,
pubmed-meshheading:15481971-RNA Replicase,
pubmed-meshheading:15481971-Rats,
pubmed-meshheading:15481971-Structure-Activity Relationship,
pubmed-meshheading:15481971-Viral Nonstructural Proteins
|
|
pubmed:year |
2004
|
|
pubmed:articleTitle |
HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.
|
|
pubmed:affiliation |
Departments of Medicinal Chemistry and Biochemistry IRBM-MRL Rome, Via Pontina, Km 30.600, 00040 Pomezia (Rome), Italy. Vincenzo_summa@merck.com
|
|
pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|
