Design and synthesis of certain substituted cycloalkanecarboxamides structurally related to safinamide with anticonvulsant potential

Design and synthesis of certain substituted cycloalkanecarboxamides structurally related to... A series of novel safinamide derivatives were synthesized and biologically evaluated for their anticonvulsant activity against maximal electroshock seizure assay and subcutaneous pentylenetetrazole (s.c. PTZ) screening test. Compound 13b is the most active derivative in s.c. PTZ screening test with an ED50 value lower than that of safinamide by about tenfold. A molecular modeling study, including fitting to sodium channel blockers 3D-pharmacophore model and docking into a branched-chain aminotransferase enzyme active site were consistent with the in vivo results. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Design and synthesis of certain substituted cycloalkanecarboxamides structurally related to safinamide with anticonvulsant potential

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Publisher
Springer Journals
Copyright
Copyright © 2013 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-013-1488-2
Publisher site
See Article on Publisher Site

Abstract

A series of novel safinamide derivatives were synthesized and biologically evaluated for their anticonvulsant activity against maximal electroshock seizure assay and subcutaneous pentylenetetrazole (s.c. PTZ) screening test. Compound 13b is the most active derivative in s.c. PTZ screening test with an ED50 value lower than that of safinamide by about tenfold. A molecular modeling study, including fitting to sodium channel blockers 3D-pharmacophore model and docking into a branched-chain aminotransferase enzyme active site were consistent with the in vivo results.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Dec 4, 2013

References

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