کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5142463 | 1496034 | 2016 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of Schiff's bases and 2-azetidinones of isonocotinyl hydrazone as potential antidepressant and nootropic agents
ترجمه فارسی عنوان
سنتز و بررسی بیولوژیکی پایه های شیف و 2-ایزیدینون های ایزونوکوتینیل هیدرازون به عنوان داروی ضد افسردگی و نوتروپیک
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی (عمومی)
چکیده انگلیسی
The synthesis and pharmacological activity of Nâ²-[(1Z)-(substituted aromatic) methylidene] pyridine-4-carbohydrazides (3a-k) and N-[3-chloro-2-(substituted aromatic)-4-oxoazetidin-1-yl]pyridine-4-carboxamides (5a-k) are described. Synthesis of 2-azetidinones was performed by novel methods of stirring and sonication involving the cyclocondensation of the appropriate Schiff's bases (3a-k) with chloroacetyl chloride, followed by the addition of triethyl amine in the presence of molecular sieves. The compounds were investigated for their antidepressant activity, compounds Nâ²-[(1Z)-(2,5-dimethoxyphenyl)methylidene]pyridine-4-carbohydrazide (3k) and N-[3-chloro-2-(2,5-dimethoxyphenyl)-4-oxoazetidin-1-yl]pyridine-4-carboxamide (5k) with 2,5-dimethoxy substitution on the aryl ring exhibited the highest antidepressant activity. In the elevated plus maze test and passive avoidance test in mice for the evaluation of nootropic activity Nâ²-[(1Z)-(4-nitrophenyl)methylidene]pyridine-4-carbohydrazide (3d) and N-[3-chloro-2-(4-nitrophenyl)-4-oxoazetidin-1-yl]pyridine-4-carboxamide (5d) with para nitro substitution on the aryl ring exhibited the highest activity. All synthesised Schiff's bases and azetidinone analogues exhibited antidepressant and nootropic activities in a dose dependant manner. The results confirmed the fact that the 2-azetidinone skeleton has potential as a CNS active agent and can be explored for the development of more potent and safe CNS active agents for therapeutic use.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Arabian Journal of Chemistry - Volume 9, Supplement 1, September 2016, Pages S79-S90
Journal: Arabian Journal of Chemistry - Volume 9, Supplement 1, September 2016, Pages S79-S90
نویسندگان
Asha B. Thomas, Rabindra K. Nanda, Lata P. Kothapalli, Sunil C. Hamane,