rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
4
|
pubmed:dateCreated |
2000-5-15
|
pubmed:abstractText |
A range of polyether para-substituted phosphoramidates were synthesised and found to have substantially elevated aqueous solubilities compared to the underivatised parent prodrug. A 30-fold increase in aqueous solubility could be achieved without a substantial decrease of in vitro activity against HIV-1. Replacement of the aryl (i.e. phenolic) moiety by tyrosine led to a substantial enhancement in aqueous solubility but also to a decrease in antiviral potency. A previously unobserved trend was identified, relating increased aryl substituent steric bulk to decreased antiviral activity.
|
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 |
21
|
pubmed:volume |
10
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
381-4
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:10714505-Amides,
pubmed-meshheading:10714505-Animals,
pubmed-meshheading:10714505-Antiviral Agents,
pubmed-meshheading:10714505-Drug Evaluation,
pubmed-meshheading:10714505-Esterases,
pubmed-meshheading:10714505-HIV-1,
pubmed-meshheading:10714505-HIV-2,
pubmed-meshheading:10714505-Liver,
pubmed-meshheading:10714505-Microbial Sensitivity Tests,
pubmed-meshheading:10714505-Phosphoric Acids,
pubmed-meshheading:10714505-Prodrugs,
pubmed-meshheading:10714505-Solubility,
pubmed-meshheading:10714505-Structure-Activity Relationship,
pubmed-meshheading:10714505-Swine,
pubmed-meshheading:10714505-Thymidine,
pubmed-meshheading:10714505-Water
|
pubmed:year |
2000
|
pubmed:articleTitle |
Enhancing the aqueous solubility of d4T-based phosphoramidate prodrugs.
|
pubmed:affiliation |
Welsh School of Pharmacy, Cardiff University, UK.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|