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Synthesis and antinociceptive activities of some pyrazoline derivatives.

机译:某些吡唑啉衍生物的合成和抗伤害作用。

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摘要

In the present study, some pyrazoline derivatives were synthesized to investigate their potential antinociceptive activities. 1-[(Benzoxazole/benzimidazole-2-yl)thioacetyl]pyrazoline derivatives were obtained by reacting 3,5-diaryl-1-(2-chloroacetyl)pyrazolines with 2-marcaptobenzoxazole/benzimidazole. The chemical structures of the compounds were elucidated by IR, (1)H NMR and FAB(+)-MS spectral data and Elemental Analyses. All of the compounds (100 mg/kg) exhibited significant antinociceptive activities in both hot plate and acetic acid-induced writhing tests. Naloxone (5 mg/kg) pre-treatment reversed the antinociceptive activities suggesting the involvement of opioid system in the analgesic actions. None of the compounds impaired motor coordination of animals when assessed in the Rota-Rod model. These results support the previous papers reporting the opioid sensitive antinociceptive activities of various benzoxazole/benzimidazole-pyrazoline derivative compounds.
机译:在本研究中,合成了一些吡唑啉衍生物以研究其潜在的抗伤害感受活性。通过使3,5-二芳基-1-(2-氯乙酰基)吡唑啉与2-巯基苯并恶唑/苯并咪唑反应获得1-[(苯并恶唑/苯并咪唑-2-基)硫代乙酰基]吡唑啉衍生物。化合物的化学结构通过IR,(1)H NMR和FAB(+)-MS光谱数据以及元素分析得到阐明。所有化合物(100 mg / kg)在热板和乙酸诱导的扭体试验中均显示出显着的抗伤害感受活性。纳洛酮(5 mg / kg)预处理逆转了抗伤害感受活性,表明阿片样物质系统参与了镇痛作用。在Rota-Rod模型中评估时,没有一种化合物会损害动物的运动协调能力。这些结果支持了以前的论文,该论文报道了各种苯并恶唑/苯并咪唑-吡唑啉衍生物化合物对阿片类药物的镇痛活性。

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