Faculty of Pharmacy, Al-Zaytoonah Private University, Amman 11733, Jordan.
Z Naturforsch C J Biosci. 2010 May-Jun;65(5-6):309-16. doi: 10.1515/znc-2010-5-601.
The N-(benzoylphenyl)-1H-indole-2-carboxamide derivatives 1-6 were synthesized, and the lipid-lowering effects of two of these novel compounds were studied using hyperlipidemic rats as an experimental model. Treatment of ethyl-1H-indole-2-carboxylate with aminobenzophenones in the presence of sodium ethoxide and DMF, followed by purification using column chromatography, gave the target compounds in good yields. The tested animals were divided into control, hyperlipidemic, compounds 2-, 3- and bezafibrate-treated groups. At a dose of 15 mg/kg body weight, compounds 2, 3 and bezafibrate significantly reduced the elevated plasma triglyceride levels after 7 and 24 h. Furthermore, the high-density lipoprotein-cholesterol levels were remarkably increased in all treated groups after 7 and 24 h compared to the hyperlipidemic control group. However, only compounds 2- and 3-treated groups obviously showed a significant reduction in plasma total cholesterol levels after 24 h. It is therefore reasonable to assume that 2 and 3 may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.
N-(苯甲酰基)苯并吲哚-2-甲酰胺衍生物 1-6 被合成出来，其中两种新型化合物的降血脂作用在高脂血症大鼠实验模型中进行了研究。在乙醇钠和 DMF 的存在下，将乙基-1H-吲哚-2-羧酸与氨基二苯甲酮反应，然后通过柱层析进行纯化，以良好的收率得到了目标化合物。将受试动物分为对照组、高脂血症组、化合物 2-、3-和苯扎贝特处理组。以 15mg/kg 体重的剂量，化合物 2、3 和苯扎贝特在 7 和 24 小时后显著降低了升高的血浆三酰甘油水平。此外，与高脂血症对照组相比，所有治疗组在 7 和 24 小时后高密度脂蛋白胆固醇水平均显著升高。然而，只有化合物 2-和 3-处理组在 24 小时后明显降低了血浆总胆固醇水平。因此，可以合理地假设 2 和 3 在治疗高脂血症和冠心病方面可能具有有前景的潜力。
