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中国药学(英文版) ›› 2017, Vol. 26 ›› Issue (11): 834-846.DOI: 10.5246/jcps.2017.11.094

• 【研究论文】 • 上一篇    下一篇

Synthesis and characterization of pyrimidines analogues as anti-Alzheimer’s agents

Yadav Rakesh*, Maan Monika, Yadav Divya   

  1. Department of Pharmacy, Banasthali University, Banasthali-304022 Rajasthan, India
  • 收稿日期:2017-05-17 修回日期:2017-06-19 出版日期:2017-11-30 发布日期:2017-09-28
  • 通讯作者: Tel.: +91-96-948-91228, E-mail: rakesh_pu@yahoo.co.in

Synthesis and characterization of pyrimidines analogues as anti-Alzheimer’s agents

Yadav Rakesh*, Maan Monika, Yadav Divya   

  1. Department of Pharmacy, Banasthali University, Banasthali-304022 Rajasthan, India
  • Received:2017-05-17 Revised:2017-06-19 Online:2017-11-30 Published:2017-09-28
  • Contact: Tel.: +91-96-948-91228, E-mail: rakesh_pu@yahoo.co.in

摘要:

Pyrimidine derivatives have been reported as neuroprotective agents useful for the treatment of various neurodegenerativedisorders. In the present study, several pyrimidine analogues have been evaluated as neuroprotective agents in Morris water maze model. It was observed that pyrimidine derivatives 817 considerably improve learning, memory, and movement deficits in animal models. Biochemical estimations of brain serum of treated animals revealed suppression of oxidative and nitrosative stress, acetylcholinesterase activity, and other parameters which leads to neurodegeneration of brain. Of all the pyrimidine derivatives, thiomorpholine derivative 8 and piperazine ethanol derivative 17 were found to be the most active neuroprotective agents and produced effects comparable to standard drug rivastigmine in terms of behavioral, biochemical, and molecular aspects.

关键词: Alzheimer’s disease, Neurodegeneration, Pyrimidine derivatives, Biochemical tests

Abstract:

Pyrimidine derivatives have been reported as neuroprotective agents useful for the treatment of various neurodegenerativedisorders. In the present study, several pyrimidine analogues have been evaluated as neuroprotective agents in Morris water maze model. It was observed that pyrimidine derivatives 817 considerably improve learning, memory, and movement deficits in animal models. Biochemical estimations of brain serum of treated animals revealed suppression of oxidative and nitrosative stress, acetylcholinesterase activity, and other parameters which leads to neurodegeneration of brain. Of all the pyrimidine derivatives, thiomorpholine derivative 8 and piperazine ethanol derivative 17 were found to be the most active neuroprotective agents and produced effects comparable to standard drug rivastigmine in terms of behavioral, biochemical, and molecular aspects.

Key words: Alzheimer’s disease, Neurodegeneration, Pyrimidine derivatives, Biochemical tests

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