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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
Epub Full Text Article
DOI: 10.2174/1570180811666140717190618      Price:  $95

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

Author(s): Suryadevara Vijayavardhini, Dandela Rambabu, Vegendla Radha, Ravikumar Kapavarapu, Mandava Venkata Basaveswara Rao and Manojit Pal
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 o-bromobenzamides 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.
Alkynes, Pd/C, coupling, 3-methyleneisoindolin-1-ones
Dr. Reddys Institute of Life Sciences University of Hyderabad Campus Hyderabad-500 046 India.