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首页> 外文期刊>Journal of Medicinal Chemistry >Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.
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Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.

机译:具有钙超载抑制作用和抗氧化活性的新型钙拮抗剂。 1.2-(3,5-二叔丁基-4-羟基苯基)-3-(氨基丙基)噻唑烷酮。

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摘要

A series of 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones was synthesized in order to explore novel calcium antagonists with potent antiischemic activity. These compounds were designed to have, in addition to Ca2+ antagonistic activity, both Ca2+ overload prevention and antioxidant activity in one molecule. These three kinds of activity were evaluated by using a K+-depolarized rat aorta, a veratridine-induced Ca2+ overload model of rat cardiomyocytes, and a soybean lipoxygenase-induced lipid peroxidation model of rabbit low-density lipoprotein, respectively. In particular, 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-[3-[N-methyl-N-[2-[3, 4-(methylenedioxy)phenoxy]ethyl]amino]propyl]-1,3-thiazolidin-4-on e (7o) was found to be highly potent and possessed a well-balanced combination of these actions in vitro.
机译:为了探索具有有效抗缺血活性的新型钙拮抗剂,合成了一系列的2-(3,5-二叔丁基-4-羟基苯基)-3-(氨基丙基)噻唑烷酮。这些化合物除具有Ca2 +拮抗活性外,还具有在一个分子中同时具有Ca2 +过载预防和抗氧化活性的功能。分别通过使用K +去极化的大鼠主动脉,维拉替丁诱导的大鼠心肌细胞Ca2 +超负荷模型和大豆脂氧合酶诱导的兔低密度脂蛋白脂质过氧化模型来评估这三种活性。特别是2-(3,5-二叔丁基-4-羟基苯基)-3- [3- [N-甲基-N- [2- [3,4-(亚甲基二氧基)苯氧基]乙基]氨基]氨基]丙基] -1,3-噻唑烷酮-4-on e(7o)具有很高的效价,并且在体外具有这些作用的良好平衡组合。

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