Suppr超能文献

某些吡唑啉衍生物的合成与抗伤害感受活性

Synthesis and antinociceptive activities of some pyrazoline derivatives.

作者信息

Kaplancikli Zafer Asim, Turan-Zitouni Gülhan, Ozdemir Ahmet, Can Ozgür v, Chevallet Pierre

机构信息

Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskişehir, Turkey.

出版信息

Eur J Med Chem. 2009 Jun;44(6):2606-10. doi: 10.1016/j.ejmech.2008.09.002. Epub 2008 Sep 12.

Abstract

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.

摘要

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,得到了1 - [(苯并恶唑/苯并咪唑 - 2 - 基)硫代乙酰基]吡唑啉衍生物。通过红外光谱、¹H核磁共振光谱和快原子轰击(+)质谱数据以及元素分析对化合物的化学结构进行了阐明。所有化合物(100毫克/千克)在热板法和醋酸诱导扭体试验中均表现出显著的抗伤害感受活性。纳洛酮(5毫克/千克)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。在转棒试验中评估时,没有一种化合物损害动物的运动协调性。这些结果支持了之前报道各种苯并恶唑/苯并咪唑 - 吡唑啉衍生物化合物具有阿片样物质敏感性抗伤害感受活性的论文。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验