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首页> 外文期刊>Archiv der Pharmazie >Some Novel Mannich Bases of 5-(3,4-Dichlorophenyl)-1,3,4-oxadiazole-2(3H)-one and Their Anti-Inflammatory Activity
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Some Novel Mannich Bases of 5-(3,4-Dichlorophenyl)-1,3,4-oxadiazole-2(3H)-one and Their Anti-Inflammatory Activity

机译：一些新的Mannich碱为5-（3,4-二氯苯基）-1,3,4-恶二唑-2（3H） - 酮和抗炎活性

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摘要

Non-steroidal anti-inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is correlated with GI toxicity related with all routine NSAIDs. Replacing this functional group with the 1,3,4-oxadiazole bioisostere is a generally used strategy to obtain an anti-inflammatory agent devoid of GI side effects. In the present work, a novel group of 5-(3,4-dichlorophenyl)-1,3,4-oxadiazole-2(3H)-one Mannich bases were synthesized and characterized on the basis of IR, H-1 NMR, and elemental analysis results. The target compounds were first tested for cytotoxicity to determine a non-toxic concentration for anti-inflammatory screening. Anti-inflammatory effects of the compounds were evaluated by in vitro lipopolysaccharide (LPS)-induced NO production and in vivo carrageenan footpad edema with ulcerogenic profile. In LPS-induced RAW 264.7 macrophages, most of the compounds showed inhibitory activity on nitrite production while compounds 5a, 5h, and 5j exhibited the best profiles by suppressing the NO production. To evaluate the in vivo anti-inflammatory potency of the compounds, the inflammatory response was quantified by increment in paw size in the carrageenan footpad edema assay. The anti-inflammatory data scoring showed that compounds 5a-d, 5g, and 5j, at the dose of 100mg/kg, exhibited anti-inflammatory activity, which for compound 5g was comparable to that of the reference drug indomethacin with 53.9% and 55.5% inhibition in 60 and 120min, respectively.
机译：非甾体抗炎药（NSAIDs）广泛用于治疗风湿性关节炎，疼痛和许多不同类型的炎症障碍，导致严重的胃肠道（GI）副作用。在其化学结构上存在的游离羧酸基团与与所有常规NSAID相关的GI毒性相关。用1,3,4-氧代唑Bioisostere替换该官能团是一种通常使用的策略，以获得缺乏GI副作用的抗炎剂。在本作工作中，在IR，H-1 NMR的基础上合成并表征了一种新的5-（3,4-二氯苯基）-1,3,4-恶二唑-2（3H） - 甘地英碱基的组合碱基组。和元素分析结果。首先测试靶化合物的细胞毒性，以确定抗炎筛选的无毒浓度。通过体外脂多糖（LPS）评估化合物的抗炎作用 - 抑制没有生产和具有溃疡性曲线的体内角叶葡萄球菌水肿。在LPS诱导的原料264.7巨噬细胞中，大多数化合物在亚硝酸盐生产上显示出抑制活性，而化合物5a，5h和5j通过抑制不产生生产表现出最佳型材。为了评价化合物的体内抗炎效力，通过卡拉胶纸脚板水肿测定中的爪子尺寸的增量量化炎症反应。抗炎数据评分显示，在100mg / kg的剂量下表现出抗炎活性的化合物5a-d，5g和5j，其用于化合物5g的抗炎活性与参考药物吲哚美辛含有53.9％和55.5分别在60和120min中抑制％。

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