Letters in Drug Design & Discovery

Author(s): Cosmas O. Okoro, John Apraku, Elisha O. Okoromoba and Olugbeminiyi O. Fadeyi

DOI: 10.2174/15701808113109990064

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Synthesis and Anticonvulsant activity of Fluorinated Cyclic Enaminones

Page: [1024 - 1031] Pages: 8

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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.