Synthesis and Evaluation of 3‐[(2,4‐Dioxo‐1,3,8‐triazaspiro[4.6]undec‐3‐yl)methyl]benzonitrile Derivatives as Potential Anticonvulsants |
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Authors: | Malavalli Madaiah Maralekere K Prashanth Hosakere D Revanasiddappa Bantal Veeresh |
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Institution: | 1. Department of Chemistry, University of Mysore, Manasagangotri, Mysore, India;2. Department of Pharmacology, G Pullareddy College of Pharmacy, Mehdipatnam, Hyderabad, India |
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Abstract: | New 3‐(2,4‐dioxo‐1,3,8‐triazaspiro4.6]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. |
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Keywords: | Anticonvulsant Maximal electroshock seizure Neurotoxicity Triazaspirobenzonitriles |
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