Nucleoside 5'-triphosphates (NTPs) play key roles in biology and medicine. However, these compounds are notoriously difficult to synthesize. We describe a one-pot method to prepare NTPs from nucleoside 5'-H-phosphonate monoesters via pyridinium phosphoramidates, and we used this approach to synthesize ATP, UTP, GTP, CTP, ribavirin-TP, and 6-methylpurine ribonucleoside-TP (6MePTP). Poliovirus RN...

Although the nucleoside analogues fludarabine and chlorodeoxyadenosine have become important therapeutic agents in chronic lymphocytic leukemia (CLL), their effectiveness is limited by drug resistance. Because such resistance is likely to result from impaired drug-induced apoptosis, it is clearly important to understand the mechanisms involved in this process. Whereas p53 can contribute to the ...

Nucleoside derivatives are important therapeutic drugs and the focal point in ongoing search for novel, more potent drug targets. In this study, a new series of pyrimidine nucleoside i.e., uridine ( 1 ) were synthesized via direct method evaluated their antimicrobial potential activity. The title compound was treated with triphenylmethyl chloride pyridine to give 5´- O -(triphenylmethyl)uridine...

Recently, 4'C-ethynyl nucleoside analogues have been identified as highly potent agents against HIV-1, including several multidrug-resistant strains. In contrast to most known nucleoside inhibitors 4'C-ethynyl nucleoside analogues possess a 3'-hydroxyl function. Here we show that the 5'O-triphosphate of 4'C-ethynyl thymidine gets readily incorporated into a nascent DNA strand by HIV-1 reverse t...

amounts of methyl incorporation. Other nucleoside triphosphates besides adenosine triphosphate were capable of sup]x>rting the incorjioration of methyl groups from L-methionine into sRNA. The nonspecificity of the nucleoside triphosphate reaction was shown to be due to an adenosine diphosphokinase reaction and not to nucleoside tri phosphate: L-methionine nucleosidyl transferase activity. Mouse...

Protozoan parasites lack the pathway of the de novo synthesis of purines and depend on host-derived nucleosides and nucleotides to salvage purines for DNA and RNA synthesis. Nucleoside hydrolase is a central enzyme in the purine salvage pathway and represents a prime target for the development of anti-parasitic drugs. The full-length cDNA for nucleoside hydrolase from Leishmania major was clone...

A variety of metabolic intermediates of the glycolytic pathway and tricarboxylic acid cycle have been found to be inhibitors of 6-phosphogluconate dehydrogenase isolated from sheep liver. All nucleoside 5’-triphosphates and 5’diphosphates are inhibitors with Ki values averaging 0.8 mM, nucleoside 5’-monophosphates are also inhibitory with Ki values averaging 6 mu. The 2’and 3’monophosphates of ...

We have developed a synthetic route for the preparation of a hybrid bisubstrate small molecule based on a nucleoside. A prototype compound was designed and docked into the catalytic domain of the AdSS enzyme bridging the region between the magnesium center of the protein to the nucleoside region. The synthesis involves coupling a brominated peptide fragment capable of complexing magnesium to a ...

The method of conjugation of a nucleoside or related compound to a carrier protein may have a significant effect on the specificity of the antibodies elicited. It is demonstrated, by means of the membrane-filtration assay, that anti-isopentenyladenosine antibodies produced by the 'periodate procedure' are much more reactive with the periodateoxidized form of the nucleoside than with the parent ...

The outbreak of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has developed into an unprecedented global pandemic. Nucleoside analogs, such as Remdesivir and Favipiravir, can serve the first-line broad-spectrum antiviral drugs by targeting viral polymerases. However, underlying mechanisms for efficacies these are far from well understood. Here, we reveal that a pyrazine derivativ...