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Aryloxy phosphoramidate triesters as pro-tides.
TLDR
The development of aryloxy phosphoramidate triesters as an effective pro-tide motif for the intracellular delivery of charged bio-active antiviral nucleoside monophosphates is described.
Characterization of the activation pathway of phosphoramidate triester prodrugs of stavudine and zidovudine.
TLDR
The rat liver phosphoramidase responsible for the formation of ddNMP was shown to be distinct from creatine kinase, alkaline phosphatase, and phosphodiesterase, thus explaining why d4T prodrugs, but not AZT pro drugs, retain anti-HIV activity in HIV-infected thymidine kinase-deficient cell cultures.
Application of the phosphoramidate ProTide approach to 4'-azidouridine confers sub-micromolar potency versus hepatitis C virus on an inactive nucleoside.
TLDR
Results confirm that phosphoramidate ProTides can deliver monophosphates of ribonucleoside analogues and suggest a potential path to the generation of novel antiviral agents against HCV infection.
Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT.
TLDR
Data strongly support the hypothesis that the AZT phosphate derivatives exert their biological effects via intracellular release of AZT nucleotide forms and suggest that the potential of nucleoside drugs in antiviral chemotherapy may be enhanced by suitable nucleotide delivery strategies.
Highly potent and selective inhibition of varicella-zoster virus by bicyclic furopyrimidine nucleosides bearing an aryl side chain.
TLDR
From a range of DNA and RNA viruses tested, only VZV was inhibited by these compounds indicating their extreme selectivity for this target virus.
Phosphoramidate ProTides of 2'-C-methylguanosine as highly potent inhibitors of hepatitis C virus. Study of their in vitro and in vivo properties.
TLDR
Systemic exposure of the ProTide and parent nucleoside are low, indicating possible low toxicity in vivo, while liver concentrations of the active species may be predictive of efficacy in the clinic, and this represents one of the most thorough cross-species studies of ProTides to date.
First example of phosphoramidate approach applied to a 4'-substituted purine nucleoside (4'-azidoadenosine): conversion of an inactive nucleoside to a submicromolar compound versus hepatitis C virus.
TLDR
Phosphoramidates achieved a significant improvement in antiviral potency over the parent nucleoside 4'-azidoadenosine with no increase in cytotoxicity.
Susceptibilities of Several Clinical Varicella-Zoster Virus (VZV) Isolates and Drug-Resistant VZV Strains to Bicyclic Furano Pyrimidine Nucleosides
TLDR
The results show that the BCNAs are far more potent inhibitors than ACV and BVDU against clinical VzV isolates as well as the VZV reference strains Oka and YS.
Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications
TLDR
This review will guide the reader through the most recent developments in this field, by considering in turn, the biological target's amenable to the action of boronic acids.
Aryloxy Phosphoramidate Triesters: a Technology for Delivering Monophosphorylated Nucleosides and Sugars into Cells
TLDR
The development of the phosphoramidate technology, mechanism of action and the application of the technology to various monophosphorylated nucleosides and sugars will be reviewed.
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