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新型苯并咪唑-2-甲酰胺衍生物的合成及体内抗高血脂活性评价

Synthesis of Novel Benzimidazole-2-carboxamide Derivatives and in Vivo Antihyperlipidemic Activity Evaluation.

作者信息

Sheikha Ghassan Abu, Bkhaitan Majdi Mohammad, Kalloush Hanin, Hamadneh Lama, Khalaf Reema Abu, Al-Qirim Tariq, Al-Hiari Yusuf

机构信息

Faculty of Pharmacy, Al-Zaytoonah University of Jordan.

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Umm Al-Qura University.

出版信息

Chem Pharm Bull (Tokyo). 2018;66(4):423-426. doi: 10.1248/cpb.c17-00908.

Abstract

Hyperlipidemia is known as an elevation of plasma lipid components. It contributes significantly to atherosclerosis which is one of the most important causative factors in cardiovascular diseases. Agents that cause a dramatic decrease in serum lipid levels are of great value in the treatment of cardiovascular diseases. For this purpose, a new series of benzimidazole propyl carboxamide benzophenone derivatives have been synthesized (7, 8, and 9). These compounds were tested in vivo to evaluate their potential hypolipidemic activity using Triton WR-1339 induced hyperlipidemic rats. All the synthesized compounds have proved to be highly biologically active, with compound 9 being the most active derivative.

摘要

高脂血症是指血浆脂质成分升高。它是动脉粥样硬化的重要促成因素,而动脉粥样硬化是心血管疾病最重要的致病因素之一。能使血清脂质水平显著降低的药物在心血管疾病治疗中具有重要价值。为此,已合成了一系列新的苯并咪唑丙基甲酰胺二苯甲酮衍生物(7、8和9)。使用Triton WR - 1339诱导的高脂血症大鼠对这些化合物进行了体内试验,以评估它们潜在的降血脂活性。所有合成化合物均已证明具有高度生物活性,其中化合物9是活性最高的衍生物。

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