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Synthesis and Studies on Antidepressant and Anticonvulsant Activities of Some 3-(2-Thienyl)pyrazoline Derivatives
Archiv der Pharmazie ( IF 5.1 ) Pub Date : 2008-11-01 , DOI: 10.1002/ardp.200800068
Zuhal Ozdemir 1 , H Burak Kandilci , Bulent Gumusel , Unsal Calis , A Altan Bilgin
Affiliation  

In this study, the synthesis of twelve 3‐(2‐thienyl)pyrazoline derivatives are described. The structures of all compounds were confirmed by UV, IR, 1H‐NMR, mass spectral data, and microanalyses. In the pharmacological studies, antidepressant and anticonvulsant activities of these compounds have been screened. The antidepressant activities of the compounds were investigated by Porsolt's behavioral despair test (forced swimming) on albino mice and compared with tranylcypromine. Among the compounds examined, the compounds 9 and 12 showed significant antidepressant activity. Anticonvulsant activities of the compounds were determined by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (metrazol) (scMet.) tests, neurotoxicities were determined by rotarod toxicity test on albino mice. Compound 8 was found to be protective against MES in the range of 30–300 mg/kg dose levels at four hours. None of the synthesized compounds showed neurotoxicity at 30–300 mg/kg dose levels.

中文翻译:

部分3-(2-噻吩基)吡唑啉衍生物抗抑郁和抗惊厥活性的合成与研究

在本研究中,描述了 12 种 3-(2-噻吩基) 吡唑啉衍生物的合成。所有化合物的结构均通过 UV、IR、1H-NMR、质谱数据和微量分析确认。在药理学研究中,已筛选出这些化合物的抗抑郁和抗惊厥活性。通过对白化小鼠的 Porsolt 行为绝望试验(强迫游泳)研究化合物的抗抑郁活性,并与反苯环丙胺进行比较。在所检测的化合物中,化合物 9 和 12 显示出显着的抗抑郁活性。化合物的抗惊厥活性通过最大电休克发作 (MES) 和皮下戊四唑 (metrazol) (scMet.) 试验确定,神经毒性通过对白化病小鼠的旋转毒性试验确定。发现化合物 8 在 30-300 mg/kg 剂量水平范围内在四小时内对 MES 具有保护作用。在 30–300 mg/kg 剂量水平下,合成的化合物均未显示神经毒性。
更新日期:2008-11-01
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