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Synthesis And Anti-Hiv Activity Of Cyclic Pyrimidine Phosphonomethoxy Nucleosides And Their Prodrugs: A Comparison Of Phosphonates And Corresponding Nucleosides

2007; Taylor & Francis; Volume: 26; Issue: 6-7 Linguagem: Inglês

10.1080/15257770701490126

1532-2335

Richard L. Mackman, Lijun Zhang, Vidya Prasad, Constantine G. Boojamra, James Chen, Janet L. Douglas, Deborah Grant, Geneviève Laflamme, Hon C. Hui, Choung U. Kim, Jay P. Parrish, Antitsa Stoycheva, S. Swaminathan, Keyu Wang, Tomáš Cihlář,

Pneumocystis jirovecii pneumonia detection and treatment

Cyclic phosphonomethoxy pyrimidine nucleosides that are bioisosteres of the monophosphate metabolites of HIV reverse transcriptase (RT) inhibitors AZT, d4T, and ddC have been synthesized. The RT inhibitory activities of the phosphonates were reduced for both dideoxy (dd) and dideoxydidehydro (d4) analogs compared to the nucleosides. Bis-isopropyloxymethylcarbonyl (BisPOC) prodrugs were prepared on selected compounds and provided > 150-fold improvements in antiviral activity.