Document Detail

Synthesis and Evaluation of 3-[(2,4-Dioxo-1,3,8-triazaspiro[4.6]undec-3-yl)methyl]benzonitrile Derivatives as Potential Anticonvulsants.
MedLine Citation:
PMID:  23335463     Owner:  NLM     Status:  Publisher    
New 3-[(2,4-dioxo-1,3,8-triazaspiro[4.6]undec-3-yl)methyl]benzonitrile derivatives 8-37 were synthesized and their pharmacological activities were determined with the objective to better understand their structure-activity relationship (SAR) for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) and pentylenetetrazole (PTZ) test. Compounds 11, 18, 31, and 32 showed significant and protective effect on seizure, when compared with the standard drug valproate. The same compounds were found to exhibit advanced anticonvulsant activity as well as lower neurotoxicity than the reference drug. From this study, it is quite apparent that there are at least three parameters for the activity of anticonvulsant drugs, that is, a lipophilic domain, a hydrophobic center, and a two-electron donor.
Malavalli Madaiah; Maralekere K Prashanth; Hosakere D Revanasiddappa; Bantal Veeresh
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-21
Journal Detail:
Title:  Archiv der Pharmazie     Volume:  -     ISSN:  1521-4184     ISO Abbreviation:  Arch. Pharm. (Weinheim)     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-21     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0330167     Medline TA:  Arch Pharm (Weinheim)     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Department of Chemistry, University of Mysore, Manasagangotri, Mysore, India.
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