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Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinson′s agents
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2008-03-28 , DOI: 10.1007/s00044-007-9074-z Shashi B. Tiwari , D. V. Kohli
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2008-03-28 , DOI: 10.1007/s00044-007-9074-z Shashi B. Tiwari , D. V. Kohli
A series of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole derivatives was prepared and their evaluation for anti-Parkinson’s activity was measured in vivo using albino rats. The result of the biological activity studies indicated that some of the synthesized compounds have good agonistic activity on the dopamine receptors and a few of them were also found to be free from neurotoxicity. Thus these compounds might be useful ligands for studying the functional role of dopamine receptors in vivo. The high log
P
value of the compounds indicates that they should easily cross the blood-brain barrier (log
P
> 2.6).
中文翻译:
3-(5-溴-2,3-二甲氧基-苯基)-[1,2,4]恶二唑类似物的合成及其作为抗帕金森氏病的评价
制备了一系列3-(5-溴-2,3-二甲氧基-苯基)-[1,2,4]恶二唑衍生物,并使用白化病大鼠在体内测量了其对帕金森氏菌活性的评估。生物学活性研究的结果表明,一些合成的化合物对多巴胺受体具有良好的激动活性,并且还发现其中一些没有神经毒性。因此,这些化合物对于研究多巴胺受体在体内的功能作用可能是有用的配体。化合物的高log P 值表明它们应轻松穿过血脑屏障(log P > 2.6)。
更新日期:2008-03-28
中文翻译:
3-(5-溴-2,3-二甲氧基-苯基)-[1,2,4]恶二唑类似物的合成及其作为抗帕金森氏病的评价
制备了一系列3-(5-溴-2,3-二甲氧基-苯基)-[1,2,4]恶二唑衍生物,并使用白化病大鼠在体内测量了其对帕金森氏菌活性的评估。生物学活性研究的结果表明,一些合成的化合物对多巴胺受体具有良好的激动活性,并且还发现其中一些没有神经毒性。因此,这些化合物对于研究多巴胺受体在体内的功能作用可能是有用的配体。化合物的高log P 值表明它们应轻松穿过血脑屏障(log P > 2.6)。