Nack, Tobias; Dinis de Oliveira, Thiago; Weber, Stefan; Schols, Dominique; Balzarini, Jan; Meier, Chris published the artcile< γ-Ketobenzyl-Modified Nucleoside Triphosphate Prodrugs as Potential Antivirals>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is antiviral nucleoside triphosphate prodrugs d4TTP HIV delivery.
The antiviral activity of nucleoside reverse transcriptase inhibitors is often hampered by insufficient phosphorylation. Nucleoside triphosphate analogs are presented, in which the γ-phosphate was covalently modified by a non-bioreversible, lipophilic 4-alkylketobenzyl moiety. Interestingly, primer extension assays using human immunodeficiency virus reverse transcriptase (HIV-RT) and three DNA-polymerases showed a high selectivity of these γ-modified nucleoside triphosphates to act as substrates for HIV-RT, while they proved to be nonsubstrates for DNA-polymerases α, β, and γ. In contrast to d4TTP, the γ-modified d4TTPs showed a high resistance toward dephosphorylation in cell extracts A series of acyloxybenzyl-prodrugs of these γ-ketobenzyl nucleoside triphosphates was prepared The aim was the intracellular delivery of a stable γ-modified nucleoside triphosphate to increase the selectivity of such compounds to act in infected vs. noninfected cells. Delivery of γ-ketobenzyl-d4TTPs was proven in T-lymphocyte cell extracts The prodrugs were potent inhibitors of HIV-1/2 in cultures of infected CEM/0 cells and more importantly in thymidine kinase-deficient CD4+ T-cells.
Journal of Medicinal Chemistry published new progress about Antiviral agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
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