一些新型 3-甲基吡唑酮衍生物的镇痛、抗炎、解热及毒理学评价。
Analgesic, anti-inflammatory, antipyretic and toxicological evaluation of some newer 3-methyl pyrazolone derivatives.
机构信息
Department of Pharmaceutical Chemistry, Himalayan Pharmacy Institute, Majhitar, Rangpo, East Sikkim 737136, India.
出版信息
Saudi Pharm J. 2011 Apr;19(2):115-22. doi: 10.1016/j.jsps.2011.01.003. Epub 2011 Jan 18.
In this paper, we described the pharmacological and toxicological studies of three pyrazolone derivatives namely PYZ1: 4-[4-N dimethylamino benzylidine]-3-methyl pyrazolin-5(4H)-one, PYZ2: 4-[2-chlorobenzylidine]-3-methylpyrazolin-5(4H)-one and PYZ3: 4-[benzylidine]-3-methylpyrazolin-5(4H)-one derivatives. Analgesic, anti-inflammatory and antipyretic studies of 3-methyl pyrazolone derivatives at 400 mg/kg, p.o. have shown significant activity as compared to control. Amongst three pyrazolone derivatives, PYZ2 was found to be more active. Based on the result of pharmacological studies, PYZ2 was selected for toxicological studies. Acute toxicity studies revealed that methyl pyrazolone derivatives are non-toxic in rats up to 5000 mg/kg, p.o. The subacute toxicity study of PYZ2 showed that decrease in Hb content, RBC and WBC count. In biochemical analysis level of blood glucose and bilirubin reduced where as AST, ALT and alkaline phosphatase level elevated. Histopathological studies revealed that there was mild toxicity on liver and kidney at 1000 mg/kg, p.o.
在本文中，我们描述了三种吡唑酮衍生物的药理学和毒理学研究，即 PYZ1：4-[4-N 二甲氨基苯亚甲基]-3-甲基吡唑啉-5(4H)-酮、PYZ2：4-[2-氯苯亚甲基]-3-甲基吡唑啉-5(4H)-酮和 PYZ3：4-[苯亚甲基]-3-甲基吡唑啉-5(4H)-酮衍生物。与对照组相比，3-甲基吡唑啉酮衍生物在 400mg/kg，po 时的镇痛、抗炎和退热研究显示出显著的活性。在三种吡唑酮衍生物中，PYZ2 的活性更高。基于药理学研究的结果，选择 PYZ2 进行毒理学研究。急性毒性研究表明，甲基吡唑啉酮衍生物在大鼠中高达 5000mg/kg，po 时是无毒的。PYZ2 的亚急性毒性研究表明，Hb 含量、RBC 和 WBC 计数减少，血糖和胆红素水平降低，而 AST、ALT 和碱性磷酸酶水平升高。组织病理学研究表明，在 1000mg/kg，po 时，肝脏和肾脏有轻度毒性。
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