Synthesis of a salacinol analogue and its alpha-glucosidase inhibitory activity / 药学学报
Acta Pharmaceutica Sinica
; (12): 647-653, 2006.
Article
de En
| WPRIM
| ID: wpr-294966
Bibliothèque responsable:
WPRO
ABSTRACT
<p><b>AIM</b>To investigate more efficient synthetic method of the nitrogen analogue 4 of salacinol (1) for searching new antidiabetic agents.</p><p><b>METHODS</b>The synthesis of the key intermediate 2, 4-O-isopropylidene-L-erythritol 1,3-cyclic sulfate (2a) was accomplished by modification of reports from D-glucose via seven steps in much more less expensive. Using this method, an efficient synthesis of 4 was carried out. The glycosidase inhibitory activity of 4 was tested for the intestinal alpha-glucosidase in vitro and compared with that of salacinol.</p><p><b>RESULTS</b>A nitrogen analogue 4 of salacinol (1) was synthesized by the coupling reaction between the cyclic sulfate 2a and an azasugar 3b.</p><p><b>CONCLUSION</b>Substitution of the sulfur atom in 1 with a nitrogen reduced the activity considerably.</p>
Texte intégral:
1
Indice:
WPRIM
Sujet Principal:
Pharmacologie
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Relation structure-activité
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Polyols
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Sulfates
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Structure moléculaire
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Chimie
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Composés de l'azote
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Antienzymes
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Alpha-Glucosidase
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Inhibiteurs des glycoside hydrolases
Limites du sujet:
Animals
langue:
En
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2006
Type:
Article