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脒基硫酮骨架在药物化学中的重要性:全面概述。

The Importance of Rhodanine Scaffold in Medicinal Chemistry: A Comprehensive Overview.

机构信息

Department of Biotechnology, Hamidiye Health Science Institute, University of Health Sciences Turkey, 34668, İstanbul, Turkey.

出版信息

Mini Rev Med Chem. 2021;21(6):738-789. doi: 10.2174/1389557521666201217144954.

Abstract

After the clinical use of epalrestat that contains a rhodanine ring, in type II diabetes mellitus and diabetic complications, rhodanin-based compounds have become an important class of heterocyclic in the field of medicinal chemistry. Various modifications to the rhodanine ring have led to a broad spectrum of biological activity of these compounds. Synthesis of rhodanine derivatives, depended on advenced throughput scanning hits, frequently causes potent and selective modulators of targeted enzymes or receptors, which apply their pharmacological activities through different mechanisms of action. Rhodanine-based compounds will likely stay a privileged scaffold in drug discovery because of different probability of chemical modifications of the rhodanine ring. We have, therefore reviewed their biological activities and structure activity relationship.

摘要

在含有雷琐辛环的依帕司他(epalrestat)临床应用之后,雷琐辛类化合物已成为医学化学领域中杂环的一个重要类别。对雷琐辛环的各种修饰导致这些化合物具有广泛的生物活性。雷二醛衍生物的合成取决于高通量扫描命中,经常导致靶向酶或受体的有效和选择性调节剂,这些调节剂通过不同的作用机制发挥其药理活性。由于雷琐辛环具有不同的化学修饰可能性,雷琐辛类化合物很可能仍然是药物发现中的一个特权支架。因此,我们综述了它们的生物活性和构效关系。

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