Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, Manojit Pal.

Graphical Abstract:


Abstract:

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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Article Details

VOLUME: 11
ISSUE: 10
Year: 2014
Page: [1188 - 1198]
Pages: 11
DOI: 10.2174/1570180811666140717190618
Price: $58