Synthesis, Computational Studies and Anticonvulsant Activity of Novel Benzothiazole Coupled Sulfonamide Derivatives
| Author | Sukhbir L. Khokra | en |
| Author | Kanika Arora | en |
| Author | Shah A. Khan | en |
| Author | Pawan Kaushik | en |
| Author | Reetu Saini | en |
| Author | Asif Husain | en |
| Issued Date | 2019-01-31 | en |
| Abstract | We report herein the synthesis of ¾ substituted benzene sulfonamides linked via phenyl ring to a benzothiazole moiety. The title compounds in the two series namely N-(4-(benzothiazole-2-yl) phenyl) 4- substituted benzene sulfonamides and N-(4-(benzothiazole-2-yl) phenyl) 3- substituted benzene sulfonamides were synthesized by condensing 2-(3/4-aminophenyl) benzothiazole with various substituted sulfonyl chlorides. The synthesized compounds were subjected to neurotoxicity screening, computational studies, and evaluation of their anticonvulsant potential. Amongst all the synthesized compounds, compound 9 emerged as the most potent anticonvulsant agent in maximal electroshock (MES) model (standard: phenytoin) in mice and showed three hydrogen bond interactions with the nicotinic acetylcholine ion gated receptors (PDB ID: 2BG9). Interestingly, compound 13 showed five hydrogen bond interactions with the target protein and thus excellent binding affinity upon computational analysis but was found to be neurotoxic. | en |
| DOI | https://doi.org/10.22037/ijpr.2019.2384 | en |
| URI | https://brieflands.com/journals/ijpr/articles/126127 | en |
| Keyword | Anticonvulsant | en |
| Keyword | Benzenesulfonamide | en |
| Keyword | Benzothiazole | en |
| Keyword | Computational analysis | en |
| Keyword | MES | en |
| Publisher | Brieflands | en |
| Title | Synthesis, Computational Studies and Anticonvulsant Activity of Novel Benzothiazole Coupled Sulfonamide Derivatives | en |
| Type | Original Article | en |
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