Synthesis and structure–activity relationship studies on novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5]decane-2,4-dione derivatives as anticonvulsant agents

A series of novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5]decane-2,4-dione derivatives 7–36 was synthesized and their pharmacological activity was determined with the objective to better understand their structure–activity relationship for anticonvulsant activity. All the compounds w...

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Bibliographic Details
Published in:Medicinal chemistry research 2013-06, Vol.22 (6), p.2633-2644
Main Authors: Madaiah, M., Prashanth, M. K., Revanasiddappa, H. D., Veeresh, B.
Format: Article
Language:English
Subjects:
Anticonvulsants
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Derivatives
Neurotoxicity
Original Research
Pharmacology/Toxicology
Phenytoin
Seizures
Sulfonamides
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Summary:A series of novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5]decane-2,4-dione derivatives 7–36 was synthesized and their pharmacological activity was determined with the objective to better understand their structure–activity relationship for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) test and their neurotoxic effects were determined by rotarod test. Majority of the compounds were active in MES tests. Compounds 24 , 27 , and 34 showed a significant and protective effect on seizure, when compared with standard drug phenytoin. The compounds having amide bond showed moderate protective effect on MES induced seizures compared to sulfonamide.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-012-0265-x