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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Pd/C-mediated Synthesis of 3-methyleneisoindolin-1-ones: Biological and Theoretical Study of their PDE4 Inhibition

Author(s): Suryadevara Vijayavardhini, Dandela Rambabu, Vegendla Anuradha, Ravikumar Kapavarapu, Mandava Venkata Basaveswara Rao and Manojit Pal

Volume 11, Issue 10, 2014

Page: [1188 - 1198] Pages: 11

DOI: 10.2174/1570180811666140717190618

Price: $65


Pd/C-Cu mediated alternative and one-pot method has been developed for the synthesis of (Z)-3- methyleneisoindolin-1-ones as potential inhibitors of PDE4. The methodology involved coupling-cyclization of obromobenzamides with a range of terminal alkynes in a single pot to afford the target compounds in acceptable yields. Some of these compounds showed encouraging inhibition of PDE4 when tested in vitro that was supported by in silico docking studies.

Keywords: Alkynes, Pd/C, coupling, 3-methyleneisoindolin-1-ones.

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