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Design, synthesis, and characterization of a series of cytochrome P(450) 3A-activated prodrugs (HepDirect prodrugs) useful for targeting phosph(on)ate-based drugs to the liver.
TLDR
The ability of a new class of phosphate and phosphonate prodrugs to effectively bypass the rate-limiting nucleoside kinase step and produce higher levels of the biologically active nucleosid triphosphate is demonstrated.
Pradefovir: a prodrug that targets adefovir to the liver for the treatment of hepatitis B.
TLDR
Tissue distribution studies in the rat showed that cyclic 1-aryl-1,3-propanyl prodrugs enhance the delivery of adefovir and its metabolites to the liver, with pradefovir exhibiting a 12-fold improvement in the liver/kidney ratio over adefavir dipivoxil.
Adenosine kinase inhibitors. 6. Synthesis, water solubility, and antinociceptive activity of 5-phenyl-7-(5-deoxy-beta-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidines substituted at C4 with glycinamides and
TLDR
To increase watersolubility, the hydrophobic C4-phenylamino substituent was replaced with a more hydrophilic group, glycinamide, and this modification resulted in improved water solubility while retaining AK inhibition potency.
Adenosine kinase inhibitors. 5. Synthesis, enzyme inhibition, and analgesic activity of diaryl-erythro-furanosyltubercidin analogues.
TLDR
This work explored the use of adenosine kinase inhibitors (AKIs) as potential antiseizure agents and demonstrated anadenosine receptor mediated therapeutic effect in the absence of overt cardiovascular side effects, and described the synthesis, enzyme inhibition structure-activity relationships, and SARs of analgesic activity of various classes of AKIs.
Adenosine kinase inhibitors. 4. 6,8-Disubstituted purine nucleoside derivatives. Synthesis, conformation, and enzyme inhibition.
TLDR
6,8-Disubstituted purine nucleosides were synthesized and evaluated as adenosine kinase inhibitors (AKIs) and proposed to bind in the anti conformation with the hydrophobic C6 and C8 substituent contributing to AK affinity in a manner similar to the C4 and C5 aryl substituents of the potent diaryltubercidin nucleoside inhibitor series.
Synthesis and Palladium-Catalyzed Cycloaddition of the Bifunctional Conjunctive Reagent Methyl (Z)-1-Methyl-2-trimethylsilylmethyl-2-butenyl Carbonate
A simple synthesis of (Z)-2-trimethylsilylmethyl-2-buten-1-ol from 2-butyn-1-ol provides ready access to disubstituted bifunctional conjunctive reagents such as the title compound. Palladium(0)
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