Synthesis of new piperidyl indanone derivatives as anticonvulsant agents

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• 作者：Nadeem Siddiqui (1)
  M. Faiz Arshad (1)
  Suroor A. Khan (1)
  Waquar Ahsan (1)
  Ruhi Ali (1)
  M. Shamsher Alam (1)
  Sharique Ahmed (2)
  
• 关键词：Indanone ; Piperidine ; Thioamide ; Anticonvulsant activity ; GABA estimation
• 刊名：Medicinal Chemistry Research
• 出版年：2012
• 出版时间：June 2012
• 年：2012
• 卷：21
• 期：6
• 页码：726-733
• 全文大小：278KB
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• 作者单位：Nadeem Siddiqui (1)
  M. Faiz Arshad (1)
  Suroor A. Khan (1)
  Waquar Ahsan (1)
  Ruhi Ali (1)
  M. Shamsher Alam (1)
  Sharique Ahmed (2)
  
  1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi, 110062, India
  2. Department of Biochemistry, Faculty of Medicine, 7th October University, Misurata, Libya
  

文摘

A series of 5,6-dimethoxy-2-{1-[arylamino/alkylamino(thioxo)methyl]-4-piperidyl-methyl}-1-indanones (4a-strong class="a-plus-plus">l) were designed and synthesized by the reaction of 5,6-dimethoxy-2-(piperidin-4-yl-methyl)-indan-1-one with aryl/alkyl isothiocyanates. The anticonvulsant activity was evaluated in animal models by maximal electroshock seizure and subcutaneous pentylenetetrazole tests. The neurotoxic effects were assessed by rotorod and ethanol potentiation tests. Gamma amino butyric acid (GABA) estimation of the selected compounds was performed in rat brain utilizing UV absorbance data. Compounds 4d, 4g, and 4j displayed encouraging anticonvulsant profile against both seizure models with remarkably lower neurotoxicity. These compounds were found to increase the GABA level in rat brain significantly.