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砜基核苷酸类似物的合成:CMP-唾液酸合成酶抑制剂的鉴定

Synthesis of sulfone-based nucleotide isosteres: identification of CMP-sialic acid synthetase inhibitors.

作者信息

Wong Jessica H, Sahni Urvashi, Li Yanhong, Chen Xi, Gervay-Hague Jacquelyn

机构信息

Department of Chemistry, University of California, Davis, One Shields Avenue, Davis, CA, USA.

出版信息

Org Biomol Chem. 2009 Jan 7;7(1):27-9. doi: 10.1039/b819155g. Epub 2008 Nov 17.

Abstract

A modular replacement approach to the synthesis of sulfo-nucleotide analogs prepared from condensation of nucleoside aldehydes with bis phosphonate Horner-Wadsworth-Emmons reagents is disclosed. These analogs were shown to be inhibitors of Neisseria meningitidis CSS (NmCSS), which is a key enzyme in the biosynthesis of the capsular polysaccharides required for bacterial infection.

摘要

公开了一种由核苷醛与双膦酸酯霍纳-沃兹沃思-埃蒙斯试剂缩合制备磺基核苷酸类似物的模块化替代方法。这些类似物被证明是脑膜炎奈瑟菌CSS(NmCSS)的抑制剂,NmCSS是细菌感染所需的荚膜多糖生物合成中的关键酶。

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