Synthesis and structure-activity relationship studies on novel 8-amino-3-2-(4-fluorophenoxy)ethyl-1,3-diazaspiro4.5decane-2,4-dione derivatives as anticonvulsant agents

Madaiah, M. and Prashanth, M. K. and Revanasiddappa, H. D. and Veeresh, B. (2013) Synthesis and structure-activity relationship studies on novel 8-amino-3-2-(4-fluorophenoxy)ethyl-1,3-diazaspiro4.5decane-2,4-dione derivatives as anticonvulsant agents. Medicinal Chemistry Research, 22 (6). pp. 2633-2644. ISSN 1554-8120

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Abstract

A series of novel 8-amino-3-2-(4-fluorophenoxy)ethyl-1,3-diazaspiro4.5 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.

Item Type:	Article
Uncontrolled Keywords:	2 chlorobenzyl 3 2 (4 fluorophenoxy)ethyl] 2, 3 diazaspiro (4.5)dec 8 yl] 3, 3 diazaspiro(4.5)dec 8 yl] 2, 3 diazaspiro(4.5)dec 8 yl] 2 bromobenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 2 cyanobenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 2 fluobenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 2 fluorobenzamide, 3 diazaspiro(4.5)dec 8 yl] 2 methylbenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 2 phenylacetamide, 3 diazaspiro(4.5)dec 8 yl] 3, 3 diazaspiro(4.5)dec 8 yl] 3 chlorobenzamide, 3 diazaspiro(4.5)dec 8 yl] 3 chlorobenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 3 fluobenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 3 fluorobenzamide, 3 diazaspiro(4.5)dec 8 yl] 3 methylbenzamide, 3 diazaspiro(4.5)dec 8 yl] 3 methylbenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 4 ethylbenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 4 fluoro 2 methyl benzenesulfonamide, 3 diazaspiro(4.5)dec 8 yl] 4 methoxybenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 4 methylbenzamide, 3 diazaspiro(4.5)dec 8 yl] 4 methylbenzene sulfonamide, 3 diazaspiro(4.5)dec 8 yl] 4 methylbenzyl sulfonamide, 3 diazaspiro(4.5)dec 8 yl] carbamate, 3 diazaspiro(4.5)dec 8 yl]benzamide, 3 diazaspiro(4.5)dec 8 yl]carbamate, 3 diazaspiro(4.5)decane 2, 4 chlorophenyl 3 2 (4 fluorophenoxy)ethyl] 2, 4 dimethyl benzenesulfonamide, 4 dione, 4 dioxo 1, 4 dioxo1, 5 dimethyl benzenesulfonamide, 5 dimethylbenzene sulfonamide, 8 amino 3 2 (4 fluorophenoxy)ethyl 1, animal experiment, animal model, anticonvulsant activity, anticonvulsive agent, article, controlled study, drug efficacy, drug synthesis, motor dysfunction, mouse, n 3 2 (4 fluorophenoxy)ethyl] 2, nonhuman, phenytoin, protection, seizure, structure activity relation, tert butyl 2, tert butyl 3 2 (4 fluorophenoxy)ethyl 2, thin layer chromatography, unclassified drug, unindexed drug
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	19 Oct 2019 07:25
Last Modified:	19 Oct 2019 07:25
URI:	http://eprints.uni-mysore.ac.in/id/eprint/9163

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