A uronic acid analogue of isofagomine lactam as a nanomolar glucuronidase inhibitor

作者：Lindback Emil; Zhou You; Lopez Oscar; Fernandez Bolanos Jose G; Pedersen Christian Marcus; Bols Mikael^*

来源：Tetrahedron Letters, 2012, 53(16): 2045-2047.

DOI：10.1016/j.tetlet.2012.02.009

• beta-Glucuronidase
• beta-Glucuronidase inhibitor
• (2,2,6,6-Tetramethyl-piperidin-1-yl)oxyl
• Bisacetoxyiodobenzene
• Selective oxidation

The synthesis of (3S,4R,5R)-3,4-dihydroxypiperidin-2-one-5-carboxylic acid ('isofagomine lactam uro-nate') from D-arabinose is reported. The product is a potent inhibitor in the low nanomolar range (K-i 36 nM) for bovine liver beta-glucuronidase.

• 出版日期2012-4-18