Design, synthesis and evaluation of carbamate-containing sialyltransferase inhibitors

doi:10.5246/jcps.2020.01.003

Abstract

Abstract:

A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linkedCMP-Neu5Ac. Their inhibitory activities were assayed against recombinant human ST3Gal I and ST6Gal I by using the Schmidt’sHPLC-based assay. The synthetic compound 15g 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.

Key words: Sialyltransferase inhibitor, Carbamate, Design, Synthesis

CLC Number:

R914

Supporting:

Wanjun Yan, Wenming Li, Decai Xiong, Xinshan Ye. Design, synthesis and evaluation of carbamate-containing sialyltransferase inhibitors[J]. Journal of Chinese Pharmaceutical Sciences, 2020, 29(1): 29-44.

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