Design, Synthesis, and In‐Vivo Pharmacological Screening of N,3‐(Substituted Diphenyl)‐5‐phenyl‐1H‐pyrazoline‐1‐carbothioamide Derivatives
Design, Synthesis, and In‐Vivo Pharmacological Screening of N,3‐(Substituted Diphenyl)‐5‐phenyl‐1H‐pyrazoline‐1‐carbothioamide Derivatives
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N,3-(取代二苯基)-5-苯基-1H-吡唑啉-1-硫代甲酰胺衍生物的设计、合成和体内药理学筛选
DOI：
10.1002/ardp.200800130
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发表时间：
2009
影响因子：
5.1
通讯作者：
W. Ahsan
中科院分区：
文献类型：
--
作者：
N. Siddiqui;Perwaiz Alam;W. Ahsan
以取代苯乙酮为原料合成了各种 3,5-(取代二苯基)-4,5-二氢吡唑-1-硫代碳酸苯酰胺。根据光谱数据确认了化合物的结构。评估了这些化合物的抗惊厥和抗抑郁活性。有趣的是，在 26 种化合物中，有 4 种（3f、3g、3t 和 3u）被发现在 25 mg/kg 的剂量下可以保护 MES 筛选中 100% 的动物。在 scPTZ 筛选中还发现它们具有明显的抗惊厥活性。与对照相比，两种化合物 3j 和 3o 在 25 mg/kg 剂量下显着缩短了不动时间的持续时间。
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.