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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.
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.
Enhanced inhibition of the EDHF phenomenon by a phenyl methoxyalaninyl phosphoramidate derivative of dideoxyadenosine
TLDR
Modifications in the lipophilicity of dideoxyadenosine and its direct intracellular delivery as a mononucleotide may enhance the ability to inhibit adenylyl cyclase and depress electrotonic signalling via myoendothelial gap junctions.
The Discovery of Potent Nonstructural Protein 5A (NS5A) Inhibitors with a Unique Resistance Profile—Part 2
TLDR
The results of the study take us a step closer towards understanding the potency of daclatasvir, a clinical candidate upon which the compounds were based, and to designing improved analogues as second‐generation antiviral agents targeting NS5A.
PHOSPHORAMIDATE DERIVATIVES OF 2′,5′-DIDEOXYADENOSINE AS POTENTIAL INHIBITORS OF THE EDHF PHENOMENON
TLDR
A new series of 2′,5′-ddA phosphoramidates has been synthesized, representing the first example ofosphoramidate protide not at the 5′-position, and successfully applied to the dideoxynucleosides.
The design, synthesis and biological evaluation of some novel phosphoramidate prodrugs
TLDR
A series of phosphoramidate derivatives of 2',3'-dideoxyadenosine was synthesised and tested as inhibitors of endothelium-derived hyperpolarizing factor EDHF, which represents the first example of the application of phosphate derivatives as non antiviral/anticancer agents.
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