Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones

European Journal of Medicinal Chemistry
I O EdafioghoBeigy Rethish

Abstract

Several cyclic enaminone esters were synthesized, characterized, and evaluated for anticonvulsant and antibacterial activities using standardized tests. A series of enaminones were mainly phenyl analogs of anticonvulsant enaminones, while a second series comprised of compounds bearing the oxazolidinone pharmacophoric moiety found in the synthetic antibacterial linezolid. The enaminone ester bearing an unsubstituted anilino analog showed class 2 anticonvulsant activity. This represents a first report of an unsubstituted anilino enaminone with anticonvulsant activity. The enaminone esters gave interesting UV data, and four analogs displayed potent anticonvulsant activities, while another four compounds showed moderate anticonvulsant activities. Surprisingly, none of the enaminone esters had any significant antibacterial activity.

Citations

Dec 18, 2010·The Journal of Pharmacology and Experimental Therapeutics·Ze-Jun WangThomas Heinbockel
Feb 26, 2014·European Journal of Medicinal Chemistry·Ivan O EdafioghoSamuel B Kombian
Dec 20, 2014·Pharmaceuticals·Thomas HeinbockelPatrice L Jackson-Ayotunde
Jun 12, 2014·The Journal of Pharmacology and Experimental Therapeutics·Charles I EzeamuzieIvan O Edafiogho

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