N',N'' -双[(E)-苯基甲基]碳二肼衍生物的高效合成及其α-胰凝乳酶抑制剂的评价

S. Iqbal, Shazia Abrar, A. Mukhtar, Irfan Ahmad, Muhammad Zawar Khan
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引用次数: 0

摘要

N′,N′′-双[(E)-苯基甲基]碳二肼是具有孤电子对的偶氮配体,在催化、医药、腐蚀、分析化学等方面有着广泛的应用。考虑到这一广泛的应用范围,我们开发了一种新的绿色快速合成N',N'' -双[(E)-苯基甲基]碳二肼及其衍生物的新方法。采用新工艺合成了一系列碳二肼1-22,收率高。所有合成的化合物都通过元素分析、1H-NMR、EI-MS和HR-MS进行了表征。这些碳二肼也用常规方法合成。通过对新方法和传统方法的比较,可以看出新开发的无溶剂方法更熟练、收率高、操作简单。由于已知蛋白酶抑制剂不仅可以抑制癌细胞系的增殖,而且还可以治疗丙型肝炎病毒和艾滋病病毒感染,因此,所有纯化和表征的化合物也被评估为它们在体外作为α-凝乳胰蛋白酶(一种酶属于蛋白酶家族)抑制剂的潜力。在所测试的化合物中,有10个化合物表现出不同程度的α-凝乳胰蛋白酶抑制潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
An Efficient Synthesis of N'',N'''-Bis[(E)-phenylmethylidene]carbonic Dihydrazide Derivatives and Their Evaluation as α-Chymotrypsin Inhibitors
N'',N'''-Bis[(E)-phenylmethylidene]carbonic dihydrazide, azotic ligands with lone electron pairs, have wide range of applications in catalysis, medicine, corrosion, and analytical chemistry. Keeping this broad range of applications in view, we have developed a new green method for the rapid synthesis of N'',N'''-Bis[(E)-phenylmethylidene]carbonic dihydrazide and its derivatives. By using a new protocol, a range of carbonic dihydrazides 1-22 has been synthesized in excellent yields. All synthesized compounds have been characterized by elemental analyses, 1H-NMR, EI-MS and HR-MS. These carbonic dihydrazides have also been synthesized via conventional method. On comparisons of new and conventional methods, it is evident that newly developed solvent-free method is more proficient, high yielding, and simple. As protease inhibitors are known to inhibit not only proliferation of cancer cell lines but also to cure hepatitis C virus and HIV aids infections, therefore, all purified and characterized compounds have also been evaluated for their potential to act as in vitro α-chymotrypsin (an enzyme belongs to protease family) inhibitors. Among tested compounds, ten compounds have shown varying degree of α-chymotrypsin inhibition potential.
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来源期刊
Kuwait Journal of Science & Engineering
Kuwait Journal of Science & Engineering MULTIDISCIPLINARY SCIENCES-
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