首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Lipid lowering activity of novel N -(benzoylphenyl)pyridine-3-carboxamide derivatives in Triton WR-1339-induced hyperlipidemic rats
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Lipid lowering activity of novel N -(benzoylphenyl)pyridine-3-carboxamide derivatives in Triton WR-1339-induced hyperlipidemic rats

机译:Triton WR-1339引起的高脂血症大鼠中新型N-(苯甲酰基苯基)吡啶-3-羧酰胺衍生物的降脂活性

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Abstract Context: Dyslipidemia is a major risk factor for the development of cardiovascular diseases. Many dyslipidemic patients do not achieve their target lipid levels with the currently available medications, and most of them may experience many side effects. Objective: The present work aimed toward identifying a new class of novel nicotinic acid-carboxamide derivatives as promising antihyperlipidemic compounds. Materials and methods: Six novel N-(benzoylphenyl)pyridine-3-carboxamide derivatives were synthesized using acid chloride pathways. All structures were confirmed using 1H-NMR, 13C-NMR, IR, and HRMS. The evaluation of biological activity was conducted using Triton WR-1339-induced hyperlipidemic rats model. Results: This study revealed that some of the newly synthesized novel N-(benzoylphenyl)pyridine-3-carboxamide derivatives mainly C4 and C6 possessed significant antihyperlipidemic activities on lipid components TG and TC (p value?Discussion and conclusion: This research opens the door for new potential antihyperlipidemic compounds derived from nicotinic acid that need further optimization of their biological activities.
机译:摘要背景:血脂异常是心血管疾病发展的主要危险因素。许多血脂异常患者无法通过目前可用的药物达到其目标脂质水平,并且其中大多数可能会遇到许多副作用。目的:目前的工作旨在鉴定一类新型的烟酸-羧酰胺衍生物作为有前途的降血脂化合物。材料和方法:使用酰基氯途径合成了六种新颖的N-(苯甲酰基苯基)吡啶-3-甲酰胺衍生物。使用 1 H-NMR, 13 C-NMR,IR和HRMS确认所有结构。使用Triton WR-1339诱导的高脂血症大鼠模型进行生物活性评估。结果:本研究表明,一些新合成的新型N-(苯甲酰基苯基)吡啶-3-甲酰胺衍生物,主要为C4和C6,对脂质组分TG和TC具有显着的降血脂活性(p值)。讨论与结论:这项研究为人们打开了大门用于衍生自烟酸的新的潜在降血脂化合物,需要进一步优化其生物活性。

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