Synthesis And Biological Activities Of 1,2,3-triazole Glycoconjugates

1,2,3-triazole compounds and their derivatives are very important five-membered heterocyclic.They are also the bioisostere for amide linkage.It has very nice stability in metabolic transformation,acid-base environment and redox reaction under high temperature.Plenty of studies discovered that 1,2,3-triazole compounds and their derivatives have good anti-HIV,anti-bacterial,hypoglycemic,anti-spasm,anti-cancer activity,it's also a good pharmacophore.Using 1,2,3-triazole ring modified existing drugs to improve the physical and chemical properties of the drugs,than enhance the biological activity of the drugs has becomed a hot topic in pharmaceutical research in recent years.Carbohydrate attracted wide attention,because of its toxicity,novel structure and good targeting.Research show that some of the biologically active group modified by sugar group can improve affinity for the drugs,reduced its toxicity,and enhanced bioavailability of the drugs.Based on 1,2,3-triazole is widely used in medicine,pesticides and polymer materials,and excellent performance of the sugar compound in medicine,than connect sugar with triazole,to obtain a compound with better performance,has become medicinal chemistry research focus.But reports in the literature is mostly based on click chemistry to synthesis 1,4-substituted 1,2,3-triazole glycoconjugates,that structure is single,and N2-substituted 1,2,3-triazole glycoconjugates has not been reported.In this paper,based on research status of 1,2,3-triazole glycoconjugates,By ‘association principle' in drug design,connect sugar with triazole with fitly design synthesized three series of 1,2,3-triazole glycoconjugates.Improve the study of 1,2,3-triazole compounds,to lay the foundation of looking for efficient 1,2,3-triazole derivatives.And the sugar groups are introduced,in order to enhance the role of the target compound of triazoles,to find 1,2,3-triazole derivatives that having effective biological activity.And part of the compounds has anti-tumor activity screening,to lay a theoretical foundation for new drug screening in further development,and has good prospects.