Jia, Xiao’s team published research in Journal of Medicinal Chemistry in 2020-06-11 | 112-63-0

Journal of Medicinal Chemistry published new progress about Anti-HIV 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.

Jia, Xiao; Schols, Dominique; Meier, Chris published the artcile< Anti-HIV-Active Nucleoside Triphosphate Prodrugs>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is HIV1 antiHIV nucleoside triphosphate d4TTP phosphorylation thymidine kinase prodrugs.

We disclose a study on nucleoside triphosphate (NTP) analogs in which the γ-phosphate is covalently modified by two different biodegradable masking units and d4T as nucleoside analog that enable the delivery of d4TTP with high selectivity in phosphate buffer (pH 7.3) and by enzyme-triggered reactions in human CD4+ T-lymphocyte CEM cell extracts This allows the bypass of all steps normally needed in the intracellular phosphorylation. These TriPPPro-nucleotides comprising an acyloxybenzyl (AB; ester) or an alkoxycarbonyloxybenzyl (ACB; carbonate) in combination with an ACB moiety are described as NTP delivery systems. The introduction of these two different groups led to the selective formation of γ-(ACB)-d4TTPs by chem. hydrolysis and in particular by cell extract enzymes. γ-(AB)-d4TTPs are faster cleaved than γ-(ACB)-d4TTPs. In antiviral assays, the compounds are highly active against HIV-1 and HIV-2 in wild-type CEM/O cells and more importantly in thymidine kinase-deficient CD4+ T-cells (CEM/TK-).

Journal of Medicinal Chemistry published new progress about Anti-HIV 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.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics