کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369179 981764 2013 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Facile synthesis of new imidazo[1,2-a]pyridines carrying 1,2,3-triazoles via click chemistry and their antiepileptic studies
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Facile synthesis of new imidazo[1,2-a]pyridines carrying 1,2,3-triazoles via click chemistry and their antiepileptic studies
چکیده انگلیسی

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 c log P values of target compounds are in the range of 3.5–5.3, which confirm their lipophilic nature.

New molecular hybrids containing imidazo[1,2-a]pyridines and 1,2,3-triazoles were synthesized and evaluated for in vivo antiepileptic as well as toxicity studies. They displayed enhanced activity in scPTZ method. The activity of 3f, 4c, 4f, 5k, 5p and 5w were comparable with standard drug diazepam.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 11, 1 June 2013, Pages 3368–3372
نویسندگان
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