Michaelidou Alia, Hadjipavlou-Litina Dimitra
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.
J Enzyme Inhib Med Chem. 2003 Dec;18(6):537-44. doi: 10.1080/14756360310001613102.
The synthesis of some new aryl acetic acids and amides and a pharmacochemical study and quantitative structure-activity relationships (QSAR) on them are described. The compounds were screened for their biological activity using the carrageenin induced rat paw oedema model and a significant inhibition of oedema occurred (44.1-80.1%) at a concentration of 0.01 mmol/1 kg. The analgesic activity, based on the inhibition of acetic acid-induced writhing in rats was also found to be significant. The compounds were found to interact with the stable free radical 1,1-diphenylhydrazyl DPPH and with DMSO (for hydroxyl radicals). The compounds were screened for radical scavenging activity with the xanthine/xanthine oxidase system for O2-* and for inhibition of soybean lipoxygenase (LOX). The results are discussed in terms of the structural and physicochemical characteristics of the compounds.
本文描述了一些新型芳基乙酸和酰胺的合成及其药物化学研究和定量构效关系(QSAR)。使用角叉菜胶诱导的大鼠足爪水肿模型筛选这些化合物的生物活性,在浓度为0.01 mmol/1 kg时出现了显著的水肿抑制(44.1 - 80.1%)。基于对大鼠乙酸诱导扭体的抑制作用,发现这些化合物的镇痛活性也很显著。发现这些化合物与稳定自由基1,1 - 二苯基肼基(DPPH)以及与二甲基亚砜(用于羟自由基)相互作用。使用黄嘌呤/黄嘌呤氧化酶系统筛选这些化合物对超氧阴离子(O2-*)的自由基清除活性以及对大豆脂氧合酶(LOX)的抑制作用。根据化合物的结构和物理化学特性对结果进行了讨论。