STUDIES ON THE SYNTHESIS OF NICOTINAMIDE NUCLEOSIDE AND NUCLEOTIDE ANALOGUES AND THEIR INHIBITIONS TOWARDS CD38 NADASE

[摘要]：Nicotinamide adenine dinucleotide (NAD) analogues inhibit the NADase activity of CD38. In the current study, efficient protocols for the synthesis of substituted-nicotinamide nucleosides and nucleotides were developed. The one-pot phosphorylation esterification strategy provides a convenient way of obtaining nicotinamide nucleoside phosphodiesters from the corresponding nucleosides. Structure activity relationship information revealed that replacement of 3'-hydroxy group with F or N(3) led to the considerably decrease of activity as compared with ara-F NMN. Phosphodiesterification of nicotinamide nucleosides lowers their inhibitory activities in some extent.

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