A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linked CMP-Neu5Ac.Their inhibitory activities were assayed against recombinant human ST3Gal I and ST6Ga...A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linked CMP-Neu5Ac.Their inhibitory activities were assayed against recombinant human ST3Gal I and ST6Gal I by using the Schmidt’s HPLC-based assay.The synthetic compound 15 g showed moderate inhibitory activity.These findings implied that carbamate might serve as a bioisosteric replacement for a phosphate group in sialyltransferase inhibitor design to improve the membrane permeability.展开更多
基金The National Key R&D Program of China(Grant No.2018YFA0507602)Project of National Science and Technology Major Project(Grant No.2019ZX09301-106)the National Natural Science Foundation of China(Grant No.91853122).
文摘A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linked CMP-Neu5Ac.Their inhibitory activities were assayed against recombinant human ST3Gal I and ST6Gal I by using the Schmidt’s HPLC-based assay.The synthetic compound 15 g showed moderate inhibitory activity.These findings implied that carbamate might serve as a bioisosteric replacement for a phosphate group in sialyltransferase inhibitor design to improve the membrane permeability.
