Synthesis of a Nitrogen Analogue of Salacinol and Its α-Glucosidase Inhibitory Activity
Synthesis of a Nitrogen Analogue of Salacinol and Its α-Glucosidase Inhibitory Activity
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Salacinol含氮类似物的合成及其α-葡萄糖苷酶抑制活性
DOI：
10.1248/cpb.49.1503
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发表时间：
2001
影响因子：
1.7
通讯作者：
M. Yoshikawa
中科院分区：
文献类型：
--
作者：
O. Muraoka;S. Ying;K. Yoshikai;Y. Matsuura;E. Yamada;T. Minematsu;G. Tanabe;H. Matsuda;M. Yoshikawa
本文合成了天然存在的磺胺离子salacinol(1)的氮类似物4，这是从印度草药Salacia reticulata中分离出来的一种有效的α-葡萄糖苷酶抑制剂，并测试了其对α-葡萄糖苷酶的抑制活性。用氮取代1中的硫原子大大降低了活性。在单晶x射线测量的基础上，确定了相关化合物(5)的固态立体结构。
A nitrogen analogue 4 of the naturally occurring sulfonium ion salacinol (1), a potent α-glucosidase inhibitor isolated from the Ayruvedic medicine Salacia reticulata, was synthesized and its inhibitory activity against α-glucosidase tested. Substitution of the sulfur atom in 1 with a nitrogen reduced the activity considerably. The solid-state stereostructure of the related compound (5) was determined on the basis of single crystal X-ray measurement.