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

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


Volume 11, 10 Issues, 2014


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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 Radha, Ravikumar Kapavarapu, Mandava Venkata Basaveswara Rao and Manojit Pal

Affiliation: Dr. Reddys Institute of Life Sciences University of Hyderabad Campus Hyderabad-500 046 India.

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 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.

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

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Article Details

Volume: 11
First Page: 1
Last Page: 11
Page Count: 11
DOI: 10.2174/1570180811666140717190618
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