New cADPR mimic 5 that integrates the simplified nucleobase and ribose was designed and synthesized by using Cu（I）-catalyzed Huisgen [3＋2] cycloaddition to build the simplified triazole nucleobase and microwave-assisted reaction to carry out intramolecular pyrophosphorylation. Primary biological investigation showed that the introduction of an ether strand to replace northern and southern riboses could retain calcium inducing activity, but the introduction of a carbon strand to replace the northern ribose could lead to decreased activity.
An optimized approach for the synthesis of N^1-ethoxymethyl-substituted cyclic inosine diphosphoribose（cIDPRE）,an analogue of cyclic adenosine diphosphoribose（cADPR）,has been developed via microwave-assisted intramolecular cyclization. The target compound has been successfully obtained through N^1-substitution,phosphorylation,cyclization and deprotection.By using this method,8-amino and bromo-substituted cIDPRE analogues were successfully obtained in good yield.The new approach has greatly shortened the synthetic route and enhanced the overall efficiency.
