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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
24
|
| pubmed:dateCreated |
1999-4-5
|
| pubmed:abstractText |
A series of novel unsymmetrical anthranilamide-containing HIV protease inhibitors was designed. The structure-activity studies revealed a series of potent P2-P3' inhibitors that incorporate an anthranilamide group at the P2' position. A reduction in molecular weight and lipophilicity is achieved by a judicious choice of P2 ligands (i.e., aromatic, heteroaromatic, carbamate, and peptidic). A systematic investigation led to the 5-thiazolyl carbamate analog 8 m, which exhibited a favorable Cmax/EC50 ratio (> 30), plasma half-life (> 8 h), and potent in vitro antiviral activity (EC50 = 0.2 microM).
|
| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Dec
|
| pubmed:issn |
0960-894X
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
15
|
| pubmed:volume |
8
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
3537-42
|
| pubmed:dateRevised |
2007-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:9934467-Amides,
pubmed-meshheading:9934467-Animals,
pubmed-meshheading:9934467-Anti-HIV Agents,
pubmed-meshheading:9934467-Cell Line,
pubmed-meshheading:9934467-HIV Protease Inhibitors,
pubmed-meshheading:9934467-Half-Life,
pubmed-meshheading:9934467-Humans,
pubmed-meshheading:9934467-Ligands,
pubmed-meshheading:9934467-Rats,
pubmed-meshheading:9934467-Structure-Activity Relationship
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
Unsymmetric nonpeptidic HIV protease inhibitors containing anthranilamide as a P2' ligand.
|
| pubmed:affiliation |
Structural Biochemistry Program, AIDS Drug Screening and Development Laboratory, SAIC-Frederick, MD, USA.
|
| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
|