TY - JOUR
T1 - Pd/C-mediated synthesis of 3-methyleneisoindolin-1-ones
T2 - Biological and theoretical study of their PDE4 inhibition
AU - Vijayavardhini, Suryadevara
AU - Rambabu, Dandela
AU - Anuradha, Vegendla
AU - Kapavarapu, Ravikumar
AU - Rao, Mandava Venkata Basaveswara
AU - Pal, Manojit
N1 - Publisher Copyright:
© 2014 Bentham Science Publishers.
PY - 2014/1/1
Y1 - 2014/1/1
N2 - 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.
AB - 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.
KW - 3-methyleneisoindolin-1-ones
KW - Alkynes
KW - Coupling
KW - Pd/C
UR - https://www.scopus.com/pages/publications/84925440831
U2 - 10.2174/1570180811666140717190618
DO - 10.2174/1570180811666140717190618
M3 - Article
AN - SCOPUS:84925440831
SN - 1570-1808
VL - 11
SP - 1188
EP - 1198
JO - Letters in Drug Design and Discovery
JF - Letters in Drug Design and Discovery
IS - 10
ER -