Abstract
A series of novel fluorinated cyclic enaminone derivatives was synthesized and evaluated as potential anticonvulsants in four animal models of epilepsy, MES, ScPTZ, rotorod neurotoxicity and 6Hz assay. Phase I screening test data indicated significant anticonvulsant activity for compounds 2a, 4a, 4b, 7 and 8. Except for 2a and 4c all the above compounds showed protection with no observed neurotoxicity. Compound 8 exhibited continuous protection at four tested time in the 6 Hz assay with no overt toxicity.
Keywords: Fluorinated cyclic, anticonvulsant, benzyl, maximal electroshock Seizure, neurotoxicity, Trifluoromethyl.
Letters in Drug Design & Discovery
Title:Synthesis and Anticonvulsant activity of Fluorinated Cyclic Enaminones
Volume: 10 Issue: 10
Author(s): Cosmas O. Okoro, John Apraku, Elisha O. Okoromoba and Olugbeminiyi O. Fadeyi
Affiliation:
Keywords: Fluorinated cyclic, anticonvulsant, benzyl, maximal electroshock Seizure, neurotoxicity, Trifluoromethyl.
Abstract: A series of novel fluorinated cyclic enaminone derivatives was synthesized and evaluated as potential anticonvulsants in four animal models of epilepsy, MES, ScPTZ, rotorod neurotoxicity and 6Hz assay. Phase I screening test data indicated significant anticonvulsant activity for compounds 2a, 4a, 4b, 7 and 8. Except for 2a and 4c all the above compounds showed protection with no observed neurotoxicity. Compound 8 exhibited continuous protection at four tested time in the 6 Hz assay with no overt toxicity.
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Okoro O. Cosmas, Apraku John, Okoromoba O. Elisha and Fadeyi O. Olugbeminiyi, Synthesis and Anticonvulsant activity of Fluorinated Cyclic Enaminones, Letters in Drug Design & Discovery 2013; 10 (10) . https://dx.doi.org/10.2174/15701808113109990064
DOI https://dx.doi.org/10.2174/15701808113109990064 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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