Synthesis and antidepressant activity of 5-(benzo[b]furan-2-ylmethyl)-6-methylpyridazin-3(2H)-one derivatives

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• 作者：Youness Boukharsa ; Bouchra Meddah…
• 关键词：Pyridazin ; 3(2H) ; one derivatives ; Antidepressant activity ; Forced swimming test (FST) ; Locomotor activity
• 刊名：Medicinal Chemistry Research
• 出版年：2016
• 出版时间：March 2016
• 年：2016
• 卷：25
• 期：3
• 页码：494-500
• 全文大小：438 KB
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• 作者单位：Youness Boukharsa (1)
  Bouchra Meddah (2)
  Ramata Yvette Tiendrebeogo (2)
  Azeddine Ibrahimi (4)
  Jamal Taoufik (1)
  Yahia Cherrah (2)
  Ali Benomar (3)
  My El Abbes Faouzi (2)
  M’hammed Ansar (1)
  
  1. Laboratory of Therapeutic Chemistry, Faculty of Medicine and Pharmacy, BP 6203, Rabat Institutes, Mohammed V University, Rabat, Morocco
  2. Laboratory of Pharmacology and Toxicology, Pharmacokinetic Research Team, Faculty of Medicine and Pharmacy, Rabat Institutes, Mohammed V University, Rabat, Morocco
  4. Biotechnology Laboratory, Faculty of Medicine and Pharmacy, Rabat Institutes, Mohammed V University, Rabat, Morocco
  3. Faculty of Medicine and Pharmacy, Research Center for Clinical Epidemiology and Therapeutic Trials, Mohammed V University, Rabat Institutes, Rabat, Morocco
  
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120

文摘

A new series of pyridazin-3-one derivatives were designed, synthesized and evaluated for their preclinical antidepressant effect on Swiss mice. Among the series, compounds 6c, 6d and 6f exhibited significant activity profile in forced swimming test. Compounds 6c and 6d were most efficacious, which at dose of 50 mg kg−1 reduced the time of immobility by 42.85 and 38.09 %, respectively, as compared to the standard drug fluoxetine which reduced the immobility time by 45.23 % at the dose of 32 mg kg−1. All the test and standard compounds were administered orally 60 min before the test. Interestingly, all active compounds did not cause any significant alteration of locomotor activity in mice as compared to control, indicating that the hybrids did not produce any motor impairment effects. The results indicate that pyridazin-3(2H)-one derivatives may have potential therapeutic value for the management of mental depression. Keywords Pyridazin-3(2H)-one derivatives Antidepressant activity Forced swimming test (FST) Locomotor activity