Zhao, Chenglong; Jia, Xiao; Schols, Dominique; Balzarini, Jan; Meier, Chris published the artcile< γ-Non-Symmetrically Dimasked TriPPPro Prodrugs as Potential Antiviral Agents against HIV>, SDS of cas: 112-63-0, the main research area is HIV antiviral prodrug; antiviral agents; bioreversible protection; nucleoside analogue; nucleoside triphosphate prodrugs; nucleotides.
Nucleoside analog reverse transcriptase inhibitors (NRTI) and nucleoside analog monophosphate prodrugs are used in combination antiretroviral therapy (cART). The design of antivirally active nucleoside triphosphate prodrugs is a recent and an important advancement in the field of nucleoside analog drug development. Here, we report on TriPPPro-derivatives of nucleoside analog triphosphates (NTPs) that comprised two different acyloxybenzyl-masks at the γ-phosphate of the NTP aiming to achieve the metabolic bypass. Thus, γ-non-sym. dimasked TriPPPro-compounds (γ-(AB,ab)-d4TTPs) were synthesized and they proved to be active against HIV-1 and HIV-2 in cultures of infected wild-type human CD4+ T-lymphocyte (CEM/0) cells and more importantly also in thymidine kinase-deficient CD4+ T-cells (CEM/TK-). From hydrolysis studies both in phosphate buffer (PB, pH 7.3) and CEM cell extracts, there was surprisingly no differentiation in the cleavage of the two acyloxybenzyl prodrug-masks. However, if within one of the two acyloxybenzyl groups a short PEG-type methoxytriglycol group was introduced, the “”standard”” acyloxybenzyl-mask was cleaved with high preference.
ChemMedChem published new progress about Anti-HIV agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics