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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1988-8-17
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pubmed:abstractText |
In an attempt to provide a derivative of 3'-azido-3'-deoxythymidine (AZT) which might be sequestered in the central nervous system and release AZT, the dihydropyridine ester 5'-(1,4-dihydro-1-methyl-3-pyridinylcarbonyl)-3'-deoxythymidine, was synthesized in a three step sequence. This material showed potent anti-HIV-1 activity in MT-4 cells most probably by hydrolysis to the parent nucleoside, AZT. This dihydropyridine derivative of AZT could be easily oxidized to a positively charged pyridinium derivative of AZT in rat brain cytosol. In turn the pyridinium form could be hydrolyzed, non-enzymatically, to AZT.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0014-5793
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
4
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pubmed:volume |
234
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
135-40
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:3164686-Acquired Immunodeficiency Syndrome,
pubmed-meshheading:3164686-Animals,
pubmed-meshheading:3164686-Brain,
pubmed-meshheading:3164686-Cell Line,
pubmed-meshheading:3164686-Chemical Phenomena,
pubmed-meshheading:3164686-Chemistry,
pubmed-meshheading:3164686-Dementia,
pubmed-meshheading:3164686-Dihydropyridines,
pubmed-meshheading:3164686-HIV,
pubmed-meshheading:3164686-Humans,
pubmed-meshheading:3164686-Male,
pubmed-meshheading:3164686-Mice,
pubmed-meshheading:3164686-Moloney murine sarcoma virus,
pubmed-meshheading:3164686-Pharmaceutical Preparations,
pubmed-meshheading:3164686-Prodrugs,
pubmed-meshheading:3164686-Rats,
pubmed-meshheading:3164686-Rats, Inbred Strains,
pubmed-meshheading:3164686-Thymidine,
pubmed-meshheading:3164686-Virus Replication,
pubmed-meshheading:3164686-Zidovudine
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pubmed:year |
1988
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pubmed:articleTitle |
AIDS dementia: synthesis and properties of a derivative of 3'-azido-3'-deoxythymidine (AZT) that may become 'locked' in the central nervous system.
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pubmed:affiliation |
Section on Biomedical Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, MD 20892.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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