4-氨基喹啉衍生物的抗伤害感受和抗炎活性的合成与评价
Synthesis and evaluation of the anti-nociceptive and anti-inflammatory activity of 4-aminoquinoline derivatives.
作者信息
de Meneses Santos Raquel, Barros Pooline Rocha, Bortoluzzi Janaína Heberle, Meneghetti Mario Roberto, da Silva Yolanda Karla Cupertino, da Silva Amanda Evelyn, da Silva Santos Mariana, Alexandre-Moreira Magna Suzana
机构信息
GCaR-Grupo de Catálise e Reatividade Química, Instituto de Química e Biotecnologia, Universidade Federal de Alagoas, Maceió, AL, Brazil.
GCaR-Grupo de Catálise e Reatividade Química, Instituto de Química e Biotecnologia, Universidade Federal de Alagoas, Maceió, AL, Brazil.
出版信息
Bioorg Med Chem. 2015 Aug 1;23(15):4390-4396. doi: 10.1016/j.bmc.2015.06.029. Epub 2015 Jun 18.
In this paper, we describe the synthesis and pharmacological evaluation of a series of 4-aminoquinolines. The compounds were characterised and tested in models of pain and inflammation, using the writhing test with acetic acid, formalin test, peritonitis test by zymosan and arthritis test with Freund's adjuvant complete assay. The results revealed that all of the 4-aminoquinolines that were prepared promoted anti-nociceptive activity as well as acute and chronic anti-inflammatory effects, with marked activity in the derivates labelled with BAQ and 7-CF3-MAQ. After 7 days of treatment, 7-CF3-MAQ did not induce significant hepatotoxicity, gastrotoxicity or nephrotoxicity.
在本文中，我们描述了一系列4-氨基喹啉的合成及药理评价。使用乙酸扭体试验、福尔马林试验、酵母聚糖诱导的腹膜炎试验以及弗氏完全佐剂关节炎试验对这些化合物进行了表征和在疼痛与炎症模型中的测试。结果显示，所制备的所有4-氨基喹啉均具有抗伤害感受活性以及急性和慢性抗炎作用，其中标记有BAQ和7-CF3-MAQ的衍生物表现出显著活性。治疗7天后，7-CF3-MAQ未诱导明显的肝毒性、胃毒性或肾毒性。
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