Linked Life Data

15715487

Source:http://linkedlifedata.com/resource/pubmed/id/15715487

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pubmed-article:15715487pubmed:abstractTextThis paper reports the synthesis and the antiviral activities of new double-prodrugs against HIV based on the known mixed SATE (S-acyl-2-thioethyl) prodrug approach. The monophosphate of the nucleoside reverse transcriptase inhibitor (NRTI) d4T was masked with one SATE group and one aromatic group through which a nonnucleoside reverse transcriptase inhibitor (NNRTI) was linked. Double-prodrug 1 was a hybrid between d4T monophosphate and the known NNRTI MKC-442, which were linked through a labile p-hydroxybenzoyl protection group in the N-3 position of MKC-442. Double-prodrugs 2 and 3 were conjugates between d4T monophosphate and the new NNRTIs 15 and 19 linked through a stable phenolic linker that was a part of the N-1 substituents of the NNRTIs. The double-prodrugs 1, 2, and 3 all had good activities against wild-type HIV-1, Y181C mutant, and also against a HIV-2 strain that was resistant to NNRTIs.lld:pubmed
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pubmed-article:15715487pubmed:dateRevised2009-8-19lld:pubmed
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pubmed-article:15715487pubmed:articleTitleSynthesis and evaluation of double-prodrugs against HIV. Conjugation of D4T with 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine)-type reverse transcriptase inhibitors via the SATE prodrug approach.lld:pubmed
pubmed-article:15715487pubmed:affiliationNucleic Acid Center, Department of Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.lld:pubmed
pubmed-article:15715487pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:15715487pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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