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ID: ALA1141999

Journal: Bioorg Med Chem Lett

Title: Biaryls and heterobiaryls as alpha-glucosidase and protein tyrosine phosphatase inhibitors.

Authors: Sharon A, Pratap R, Tripathi B, Srivastava AK, Maulik PR, Ram VJ.

Abstract: Various 6-aryl-4-substituted-2H-pyran-2-one-3-carbonitriles (1a-d) have been synthesized as precursor for the synthesis of 3,4-dihydro-1H-isothiochroman (2a) and benzocycloalkanes (2b-e). Highly functionalized 9-thiaphenanthrene (3b) and phenanthrene (3a) have also been obtained from the reaction of 1c with thiochroman-4-one and 1-tetralone separately. Similarly 4 has been obtained by the ring transformation of 1d by 4-trifluoromethylacetophenone. Most of the synthesized compounds were evaluated for alpha-glucosidase and protein tyrosine phosphatase inhibitory activities. Some of the compounds, 2a, 3a and b and 4 displayed better alpha-glucosidase inhibitory activity compared to standard drug acarbose.

CiteXplore: 15713383

DOI: 10.1016/j.bmcl.2005.01.036