Pd/C-mediated Synthesis of 3-methyleneisoindolin-1-ones: Biological and Theoretical Study of their PDE4 Inhibition
Letters in Drug Design & Discovery,
Suryadevara Vijayavardhini, Dandela Rambabu, Vegendla Anuradha, Ravikumar Kapavarapu, Mandava Venkata Basaveswara Rao and Manojit PalAffiliation:
Dr. Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Hyderabad-500 046, India.
AbstractPd/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.
Alkynes, Pd/C, coupling, 3-methyleneisoindolin-1-ones.
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