Literature DB >> 23623419

Facile synthesis of new imidazo[1,2-a]pyridines carrying 1,2,3-triazoles via click chemistry and their antiepileptic studies.

Shrikanth Ulloora1, Ramakrishna Shabaraya, Airody Vasudeva Adhikari.   

Abstract

The present article reports the synthesis and anticonvulsant studies of new 2-arylimidazo[1,2-a]pyridines carrying suitably substituted 1,2,3-triazoles as well as their intermediates. The structures of newly synthesized compounds were confirmed by various spectroscopic techniques. The anticonvulsant study was carried out by MES and scPTZ screening methods, while their toxicity study was performed following Rotarod method. The active compounds showed enhanced seizure control in scPTZ method when compared with that of MES method. Compounds 3f, 4c, 4f, 5k, 5p and 5w carrying active pharmacophores exhibited complete protection against seizure and their results were comparable with standard drug diazepam. Majority of new compounds were found to be non-toxic, while few of them showed toxicity at 100 mg/kg. The clogP values of target compounds are in the range of 3.5-5.3, which confirm their lipophilic nature.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23623419     DOI: 10.1016/j.bmcl.2013.03.086

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Urea-thiazole/benzothiazole hybrids with a triazole linker: synthesis, antimicrobial potential, pharmacokinetic profile and in silico mechanistic studies.

Authors:  Nisha Poonia; Kashmiri Lal; Ashwani Kumar; Anil Kumar; Srikanta Sahu; Anurag T K Baidya; Rajnish Kumar
Journal:  Mol Divers       Date:  2021-10-20       Impact factor: 3.364

2.  Ι₂-mediated amination/cyclization of ketones with 2-aminopyridines under high-speed ball milling: solvent- and metal-free synthesis of 2,3-substituted imidazo[1,2-a]pyridines and zolimidine.

Authors:  Fang-Jian Wang; Hui Xu; Ming Xin; Ze Zhang
Journal:  Mol Divers       Date:  2016-03-14       Impact factor: 2.943

3.  Synthesis, Characterization, and Enzyme Inhibition Properties of 1,2,4-Triazole Bearing Azinane Analogues.

Authors:  Hafiz Muhammad Abdullah Asif; Shagufta Kamal; Aziz-Ur Rehman; Shahid Rasool; Muhammad Sajid Hamid Akash
Journal:  ACS Omega       Date:  2022-09-01

Review 4.  Triazole analogues as potential pharmacological agents: a brief review.

Authors:  Sachin Kumar; Sukhbir Lal Khokra; Akash Yadav
Journal:  Futur J Pharm Sci       Date:  2021-05-25

Review 5.  Recent developments on triazole nucleus in anticonvulsant compounds: a review.

Authors:  Ming-Xia Song; Xian-Qing Deng
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

  5 in total

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