Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants

[Display omitted] •Various reports on anticonvulsant potential of nitrogen containing heterocycles influenced researchers to design newer synthetic strategies.•Various synthetic strategies reported by different research groups for nitrogen containing heterocyclic classes have been summarized in this...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2020-08, Vol.28 (15), p.115585-115585, Article 115585
Hauptverfasser: Grover, Gourav, Nath, Rajarshi, Bhatia, Rohit, Akhtar, Md Jawaid
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Sprache:eng
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Zusammenfassung:[Display omitted] •Various reports on anticonvulsant potential of nitrogen containing heterocycles influenced researchers to design newer synthetic strategies.•Various synthetic strategies reported by different research groups for nitrogen containing heterocyclic classes have been summarized in this compilation.•Preclinical data for the anticonvulsant potential of synthesized derivatives is described in a comparison with standard marketed drugs.•Structural activity relationship has also been discussed for various chemical classes of synthesized derivatives. Epilepsy is one of the commonly prevailing neurological disorders. According to the reports, it is evident that about 80% of the epileptic cases have been observed in developing countries. Although there are many drugs with significant potency available in the market; still there is an issue of selectivity and toxicity. Therefore, continuous attempts have been made by the researchers to develop newer therapeutic agents against epilepsy. Many synthetic strategies have been available in the literature to synthesize various classes of anticonvulsants with promising activity. In the presented review, authors have summarized some newer synthetic routes being used for the synthesis of nitrogen-containing anticonvulsants taking a cue from the reported established anticonvulsant drugs viz. vigabatrin, sodium valproate, oxcarbazepine, felbamate, retigabine, and gabapentin. Various derivatives with the substitution for better anticonvulsant profile have been described in the figures for easy comparative study. The structure–activity relationship (SAR) of compounds with maximum potency has also been discussed. This article may serve as a boost for the researchers to modify the pre-existing synthetic routes as well as to improve potency and yield of the compounds.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2020.115585