| Literature DB >> 19282192 |
Joanna Romanowska1, Agnieszka Szymańska-Michalak, Jerzy Boryski, Jacek Stawiński, Adam Kraszewski, Roberta Loddo, Giuseppina Sanna, Gabriella Collu, Barbara Secci, Paolo La Colla.
Abstract
Di-aryl nucleoside phosphotriesters have been explored as a new type of pronucleotides for the purpose of anti-HIV-1 therapy and efficient synthetic protocols, based on H-phosphonate chemistry, have been developed for the preparation of this class of compounds. It was found that anti-HIV-1 activity of the phosphotriesters bearing an antiviral nucleoside moiety (AZT, ddA) and also ddU was due, at least partially, to intracellular conversion into the corresponding nucleoside 5'-monophosphates, and their efficiency correlated well with the pK(a) values of the aryloxy groups present.Entities:
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Year: 2009 PMID: 19282192 DOI: 10.1016/j.bmc.2009.02.033
Source DB: PubMed Journal: Bioorg Med Chem ISSN: 0968-0896 Impact factor: 3.641