Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
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 and Manojit Pal

Affiliation: Dr. Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Hyderabad-500 046, India.

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

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.

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Article Details

VOLUME: 11
ISSUE: 10
Page: [1188 - 1198]
Pages: 11
DOI: 10.2174/1570180811666140717190618