期刊
ACS CATALYSIS
卷 8, 期 1, 页码 43-47出版社
AMER CHEMICAL SOC
DOI: 10.1021/acscatal.7b03257
关键词
biocatalysis; enzymatic synthesis; Neu5Ac2en; sialidase; sialidase inhibitor
资金
- National Institutes of Health (NIH) [U01GM120419]
- NIH [R01AI130684]
Sialidase transition-state analogue inhibitor 2,3-dehydro-2-deoxy-N-acetylneuraminic acid (Neu5Ac2en, DANA) has played a leading role in developing clinically used anti-influenza virus drugs. Taking advantage of the Neu5Ac2en-forming catalytic property of Streptococcus pneumoniae sialidase SpNanC, an effective one-pot multienzyme (OPME) strategy has been developed to directly access Neu5Ac2en and its C-5, C-9, and C-7-analogues from Nacetylmannosamine (ManNAc) and analogues. The obtained Neu5Ac2en analogues can be further derivatized at various positions to generate a larger inhibitor library. Inhibition studies demonstrated improved selectivity of several C-5- or C-9-modified NeuSAc2en derivatives against several bacterial sialidases. The study provides an efficient enzymatic method to access sialidase inhibitors with improved selectivity.
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