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Synthesis of novel mono and bis-indole conduritol derivatives and their α/β-glycosidase inhibitory effects.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Dec 15; Vol. 22 (24), pp. 7499-503. Date of Electronic Publication: 2012 Oct 23. - Publication Year :
- 2012
-
Abstract
- Here we synthesized four novel indole conduritol derivatives 1-4 for the first time in the literature and probed their biological activities with the α and β-glucosidases. The compounds showed quite effective glucosidase inhibitory action. IC(50) values of the compounds were compared with the known glucosidase inhibitor acarbose and it was determined that newly synthesized indole conduritols had more powerful effect against β-glucosidase in addition to exhibiting moderate influence against α-glucosidase. Our molecules thus constitute an important starting point for the design and exploitation of novel glucosidase inhibitors since glucosidase inhibitors have widespread applications in the treatment of diabetes, viral infections, lysosomal storage diseases and cancers.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Dose-Response Relationship, Drug
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Glycoside Hydrolases metabolism
Indoles chemical synthesis
Indoles chemistry
Inositol analogs & derivatives
Inositol chemical synthesis
Molecular Structure
Structure-Activity Relationship
Enzyme Inhibitors pharmacology
Glycoside Hydrolases antagonists & inhibitors
Indoles pharmacology
Inositol pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 23137433
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.10.038