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Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Apr 15; Vol. 16 (8), pp. 2139-43. Date of Electronic Publication: 2006 Feb 07. - Publication Year :
- 2006
-
Abstract
- PTPases are considered to be involved in the etiology of diabetes mellitus and neural diseases, such as Alzheimer's disease and Parkinson's disease. Therefore, PTPase inhibitors should be useful tools to study the role of PTPases in these diseases and other biological phenomena, and which can be developed into chemotherapeutic agents. In the present study, we have synthesized novel benzofuran isoxazolines 13-21 via 1,3-dipolar cycloaddition reaction using karanjin (1) and kanjone (2), isolated from Pongamia pinnata fruits. All the synthesized compounds were evaluated against PTPase enzyme. Compounds 19 and 20 displayed significant inhibitory activity with IC50 values 76 and 81 microM, respectively.
- Subjects :
- Benzofurans chemical synthesis
Benzofurans pharmacology
Benzopyrans chemistry
Drug Design
Enzyme Inhibitors pharmacology
Hypoglycemic Agents pharmacology
Isoxazoles chemical synthesis
Isoxazoles pharmacology
Millettia chemistry
Models, Chemical
Oxazolone analogs & derivatives
Oxazolone chemical synthesis
Oxazolone pharmacology
Protein Binding
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Enzyme Inhibitors chemical synthesis
Hypoglycemic Agents chemical synthesis
Protein Tyrosine Phosphatases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16460930
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.01.062