کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1254474 971376 2016 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of novel dicarbonylalkyl piperazine derivatives as neuroprotective agents
ترجمه فارسی عنوان
طراحی، سنتز و ارزیابی بیولوژیکی مشتقات Dicarbonylalkyl piperazine جدید به عنوان عوامل محافظت کننده نوروپاتی
کلمات کلیدی
Dicarbonylalkyl piperazine؛ نوروپروتئین؛ سکته مغزی ایسکمیک
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی (عمومی)
چکیده انگلیسی

In the search of novel neuroprotective agents with higher potency than our previously identified anti-ischemic stroke drug candidate 1, a series of novel dicarbonyl piperazine derivatives were synthesized and evaluated on their neuroprotective activity via oxygen–glucose deprivation test in the neuron-like PC12 cells, hypoxia tolerance model in mice and focal cerebral ischemia model in rats. The result obtained indicated that compounds 7f, 7k and 7o, exhibited neuroprotective activity. Particularly, compound 7o containing 2,5-dimethylpiperazin moiety, showed prolonged life time of mice and reduced cerebral infarction of rats, which provided a potential candidate for the development of neuroprotective agents.

Methyl or methoxy introduction compounds like 7o or 7f provided higher anti-ischemic stroke activity than lead compound 1, while methylene introduction compounds like 7b, 7e and 7r showed loss of activity.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chinese Chemical Letters - Volume 27, Issue 3, March 2016, Pages 387–390
نویسندگان
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