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N,3-(取代二苯基)-5-苯基-1H-吡唑啉-1-碳硫代酰胺衍生物的设计、合成及体内药理筛选

Design, synthesis, and in-vivo pharmacological screening of N,3-(substituted diphenyl)-5-phenyl-1H-pyrazoline-1-carbothioamide derivatives.

作者信息

Siddiqui Nadeem, Alam Perwaiz, Ahsan Waquar

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi, India.

出版信息

Arch Pharm (Weinheim). 2009 Mar;342(3):173-81. doi: 10.1002/ardp.200800130.

Abstract

Various 3,5-(substituted diphenyl)-4,5-dihydro-pyrazole-1-carbothioic acid phenylamides were synthesized starting from substituted acetophenones. Structures of the compounds were confirmed on the basis of spectral data. The compounds were evaluated for their anticonvulsant and antidepressant activity. Interestingly, out of 26 compounds, four (3f, 3g, 3t, and 3u) were found to protect 100% of the animals in the MES screen at a dose of 25 mg/kg. They were also found to have appreciable anticonvulsant activity in scPTZ screen. Two compounds, 3j and 3o, significantly reduced the duration of the immobility time at 25 mg/kg dose, when compared to control.

摘要

从取代苯乙酮出发合成了各种3,5 -(取代二苯基)-4,5 -二氢吡唑-1 -碳硫代酸苯酰胺。根据光谱数据确定了化合物的结构。对这些化合物的抗惊厥和抗抑郁活性进行了评估。有趣的是,在26种化合物中,有4种(3f、3g、3t和3u)在25 mg/kg剂量下在最大电休克(MES)筛选中能保护100%的动物。它们在皮下注射戊四氮(scPTZ)筛选中也具有明显的抗惊厥活性。与对照组相比,两种化合物3j和3o在25 mg/kg剂量下显著缩短了不动时间的持续时间。

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