Evaluation of the analgesic activity of new derivatives of aryl propionic acid on gastric male mice

Sadiq Al-Mansury, Suhad J. Hadi, Nabah H. Checkor, Mohammed J. Jawad, Hussein A. Ghanimi, Adnan M. Jassim, Hawraa T. Abass, Rusul Heider, Hamzah H. Kzar, Moaed E. Al-Gazally
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Abstract

This study focused on the recent synthesis of new compounds from aryl propionic acid derivatives compared to naproxen. The present study aimed to investigate the safety and efficiency of the new derivatives in improving analgesic effects and reducing adverse effects via modifying its chemical structure by adding new functional groups. The new compounds were characterized, and evaluate their pharmacodynamic effects. The analysis and characterization of new compounds were by 1HMNR and FT-IR spectrum. The investigation of the adverse effect after 5 days of remedy with 20 mg/kg daily administered with naproxen derivatives to the healthy male albino mice (25-30 g) for analgesic activity using the hot plate method. Mice were parted into 5 groups, consisting of the control group and 4 groups that administered naproxen or derivatives of aryl propionic acid (E, H, D1 and D2). The main tests are done by a hot plate, biochemical, macroscopic, and microscopic inspection. The results confirmed that the new drugs have potent analgesic activity. The results showed that mice administered with D1 expressed less ulcerative effect than parent naproxen, H, E and ethanol. Moreover, the number of lesions was significantly less in the D2 group, while D1-treated mice recorded no evidence of ulcers or hemorrhage in their stomachs after being examined under a dissecting microscope. The study concluded that the new D1 derivative is a compound worthy of research and future clinical applications due to its relatively high efficacy and low adverse effects compared to other derivatives prepared and tested in this study. Keywords: Analgesic, Aryl propionic acid, Naproxen, Acidity
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芳基丙酸新衍生物对胃雄性小鼠的镇痛作用评价
本文研究了近年来与萘普生相比,芳基丙酸衍生物合成的新化合物。本研究旨在通过添加新的官能团改变其化学结构,研究新衍生物在改善镇痛效果和减少不良反应方面的安全性和有效性。对新化合物进行了表征,并对其药效学效果进行了评价。用1HMNR和FT-IR对新化合物进行了分析和表征。用热板法观察健康雄性白化小鼠(25 ~ 30 g)口服萘普生衍生物20 mg/kg / d后的不良反应。将小鼠分为5组,分别为对照组和萘普生或芳基丙酸衍生物(E、H、D1、D2)组。主要检测方法有热板、生化、宏观和显微检查。结果证实新药具有强效镇痛作用。结果表明,给药小鼠D1无表达的溃疡效果优于给药小鼠萘普生、H、E和乙醇。此外,D2组的病变数量明显减少,而d1组的胃在解剖显微镜下检查后,没有记录到溃疡或出血的证据。本研究认为,与本研究制备和测试的其他衍生物相比,新的D1衍生物具有相对较高的疗效和较低的不良反应,值得研究和未来临床应用。关键词:镇痛药,芳基丙酸,萘普生,酸度
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