Heterocycles p. 2837 - 2850 (2011)
Update date:2022-08-05
Topics: Chemical Synthesis Structure-Activity Relationship (SAR) Studies Biological Studies Clinical Implications
Chen, Zhe
Kwong, Anna Ka Yee
Yang, Zhenjun
Zhang, Liangren
Lee, Hon Cheung
Zhang, Lihe
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 N3 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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