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Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ahmad G,Mishra PK,Gupta P,Yadav PP,Tiwari P,Tamrakar AK,Srivastava AK,Maurya R

doi

10.1016/j.bmcl.2006.01.062

subject

Has Abstract

pub_date

2006-04-15 00:00:00

pages

2139-43

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00091-6

journal_volume

16

pub_type

杂志文章

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