Y. Kobayashi et M. Shiozaki, SYNTHETIC STUDIES OF NOVEL TREHALASE INHI BITOR, TREHAZOLIN AND ITS RELATED-COMPOUNDS, Yuki Gosei Kagaku Kyokaishi, 54(4), 1996, pp. 300-310
Total synthesis of the novel trehalase inhibitor, trehazolin was accom
plished, and its absolute structure was determined. On the basis of th
is synthetic study, several related compounds including its stereoisom
ers were synthesized to investigate the effects of their stereochemist
ry and framework on the enzyme inhibitory activities. Further studies
were carried out for the syntheses and biological evaluation of the tr
ehazolin derivatives, which were derived from its natural aminocyclito
l and modified at the terminal amino group of trehalamine. They were d
esigned as compounds exhibiting the inhibition toward the other glucos
idases such as intestinal maltase and isomaltase, judging from the str
uctural similarity between D-glucose and trehalamine.