Synthesis and Evaluation of Bicyclo[3.1.0]hexane-Based UDP-Galf Analogues as Inhibitors of the Mycobacterial Galactofuranosyltransferase GlfT2

Lowary, Todd L. ¹Li, Jing²

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作者信息

1. Univ Alberta, Dept Chem, 11227 Saskatchewan Dr, Edmonton, AB T6G 2G2, Canada
2. Heilongjiang Bayi Agr Univ, Coll Life Sci & Technol, Daqing 163319, Heilongjiang Pr, Peoples R China
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Abstract

UDP-galactofuranose (UDP-Galf) is the donor substrate for both bifunctional galactofuranosyltransferases, GlfT1 and GlfT2, which are involved in the biosynthesis of mycobacterial galactan. In this paper, a group of UDP-Galf mimics were synthesized via reductive amination of a bicyclo[3.1.0]hexane-based amine by reacting with aromatic, linear, or uridine-containing aldehydes. These compounds were evaluated against GlfT2 using a coupled spectrophotometric assay, and were shown to be weak inhibitors of the enzyme.

Key words

mycobacteria/tuberculosis/galactofuranosyltransferases/UDP-Galf/inhibitors/reductive amination

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出版年

2016

Molecules

SCI

ISSN：1420-3049

被引量2

参考文献量31

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