2. Academic Validation
  3. Synthesis of novel benzofuran isoxazolines as protein tyrosine phosphatase 1B inhibitors

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

  • Bioorg Med Chem Lett. 2006 Apr 15;16(8):2139-43. doi: 10.1016/j.bmcl.2006.01.062.
Ghufran Ahmad 1,  Pushpesh K Mishra,  Prasoon Gupta,  Prem P Yadav,  Priti Tiwari,  Akhilesh K Tamrakar,  Arvind K Srivastava,  Rakesh Maurya
Affiliations

Affiliation

  • 1 Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
PMID: 16460930 DOI: 10.1016/j.bmcl.2006.01.062
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.

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