Source:http://linkedlifedata.com/resource/pubmed/id/12767599
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
|
pubmed:dateCreated |
2003-5-27
|
pubmed:abstractText |
A first series of novel bishydroxymethyl-substituted cage dimeric 4-aryl-1,4-dihydropyridines 5-8 has been synthesised and evaluated as HIV-1 protease and HIV-inhibitors in vitro assays. Moderate activity data of protease inhibition have been found for of the N-Boc substituted compound 8. Reduced activity for compound 6 and almost no residual activity of 5 and 7 emphasise the importance of the tert. butyl substituent for protease inhibitory activity thus supporting a discussed probable binding of the N-acyloxy substituent to the S2/S2' regions of protease.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0223-5234
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
38
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
495-9
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:12767599-Dihydropyridines,
pubmed-meshheading:12767599-Dimerization,
pubmed-meshheading:12767599-Drug Evaluation, Preclinical,
pubmed-meshheading:12767599-HIV Protease Inhibitors,
pubmed-meshheading:12767599-HIV-1,
pubmed-meshheading:12767599-Inhibitory Concentration 50,
pubmed-meshheading:12767599-Structure-Activity Relationship
|
pubmed:year |
2003
|
pubmed:articleTitle |
Structure-activity relationships of first bishydroxymethyl-substituted cage dimeric 4-aryl-1,4-dihydropyridines as HIV-1 protease inhibitors.
|
pubmed:affiliation |
Department of Pharmacy, Martin-Luther-University Halle-Wittenberg, Wolfgang-Langenbeck-Strasse 4, 06120 Halle, Germany. hilgeroth@pharmazie.uni-halle.de
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|